Amitriptyline
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|
| Systematic (IUPAC) name |
| 3-(10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-ylidene)-N,N-dimethylpropan-1-amine |
| Clinical data |
| Trade names |
Tryptomer, Elavil |
| AHFS/Drugs.com |
monograph |
| MedlinePlus |
a682388 |
| Pregnancy cat. |
D (US) |
| Legal status |
℞ Prescription only |
| Routes |
Oral |
| Pharmacokinetic data |
| Bioavailability |
30–60% due to first pass metabolism |
| Protein binding |
> 90% |
| Metabolism |
Hepatic
CYP2C19, CYP1A2, CYP2D6 |
| Half-life |
10–50 hours, with an average of 15 hours |
| Excretion |
Renal |
| Identifiers |
| CAS number |
50-48-6 Y
549-18-8 (hydrochloride) |
| ATC code |
N06AA09 |
| PubChem |
CID 2160 |
| IUPHAR ligand |
200 |
| DrugBank |
DB00321 |
| ChemSpider |
2075 Y |
| UNII |
1806D8D52K Y |
| KEGG |
D07448 Y |
| ChEBI |
CHEBI:2666 Y |
| ChEMBL |
CHEMBL629 Y |
| Chemical data |
| Formula |
C20H23N |
| Mol. mass |
277.403 g/mol |
SMILES
- c3cc2c(/C(c1c(cccc1)CC2)=C\CCN(C)C)cc3
|
InChI
-
InChI=1S/C20H23N/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h3-6,8-12H,7,13-15H2,1-2H3 Y
Key:KRMDCWKBEZIMAB-UHFFFAOYSA-N Y
|
Y (what is this?) (verify)
|
Amitriptyline (Tryptomer, Elavil, Tryptizol, Laroxyl, Sarotex, Lentizol, Endep) is a tricyclic antidepressant (TCA). It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs according to a study from early 2001.[1] As well as reducing depressive symptoms, these types of tricyclics also ease migraines, tension headaches, anxiety attacks and some schizophrenic symptoms. It is also known to reduce aggression and violent behaviour.
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Contents
- 1 Medical uses
- 2 Adverse effects
- 3 Pharmacology
- 4 History
- 5 See also
- 6 References
- 7 Further reading
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Medical uses
Amitriptyline is used for a number of medical conditions including: depressive disorders, anxiety disorders, attention deficit hyperactivity disorder, migraine prophylaxis, eating disorders, bipolar disorder, post-herpetic neuralgia, and insomnia.[2]
Amitriptyline is used in ankylosing spondylitis for pain relief. It is also used as a preventive for patients with recurring biliary dyskinesia (sphincter of Oddi dysfunction).[3]
Amitriptyline is also used in the treatment of nocturnal enuresis in children.[4]
Amitriptyline may be prescribed for other conditions such as cyclic vomiting syndrome post-traumatic stress disorder (PTSD),[5] chronic pain, tinnitus, chronic cough, carpal tunnel syndrome (CTS), fibromyalgia, vulvodynia, interstitial cystitis, male chronic pelvic pain syndrome, irritable bowel syndrome (IBS), diabetic peripheral neuropathy, neurological pain, laryngeal sensory neuropathy, chronic fatigue syndrome and painful paresthesias related to multiple sclerosis. Typically lower dosages are required for pain modification of 10 to 50 mg daily.[6]
A randomized controlled trial published in June 2005 found that amitriptyline was effective in functional dyspepsia that did not respond to a first-line treatment (famotidine or mosapride).[7]
Adverse effects
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This section needs additional citations for verification. (May 2010) |
The main two side effects that occur from taking amitriptyline are drowsiness and a dry mouth. Other common side effects of using amitriptyline are mostly due to its anticholinergic activity, including: weight gain, changes in appetite, muscle stiffness, nausea, constipation, nervousness, dizziness, blurred vision, urinary retention, and changes in sexual function. Some rare side effects include seizures, tinnitus, hypotension, mania, psychosis, sleep paralysis, hypnagogic or hypnopompic hallucinations related to sleep paralysis, heart block, arrhythmias, lip and mouth ulcers, extrapyramidal symptoms, depression, tingling pain or numbness in the feet or hands, yellowing of the eyes or skin, pain or difficulty passing urine, confusion, abnormal production of milk in females, breast enlargement in both males and females, fever with increased sweating, and suicidal thoughts.[8] The Indianapolis Discovery Network for Dementia (IDND) [9] rates Amitriptyline as having definite 'Anticholinergic Effects'. A side effect of many commonly used drugs with such effects appears to be to increase the risks of both cognitive impairment and death in older people, according to new research led by the University of East Anglia (UEA).[10] Amitriptyline can induce hepatotoxicity.[11]
Overdose
Main article: Tricyclic antidepressant overdose
The symptoms and the treatment of an overdose are largely the same as for the other TCAs. The British National Formulary notes that Amitryptyline can be particularly dangerous in overdose,[12] thus it and other tricyclic antidepressants are no longer recommended as first line therapy for depression. Alternative agents, SSRIs and SNRIs are safer in overdose, though they are no more efficacious than TCAs.
Pharmacology
Amitriptyline acts primarily as a serotonin-norepinephrine reuptake inhibitor, with strong actions on the serotonin transporter and moderate effects on the norepinephrine transporter.[13][14] It has negligible influence on the dopamine transporter and therefore does not affect dopamine reuptake, being nearly 1,000 times weaker on it than on serotonin.[14]
Amitriptyline additionally functions as a 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, H1, H2,[15] H4,[16][17] and mACh receptor antagonist, and σ1 receptor agonist.[18][19][20][21] It has also been shown to be a relatively weak NMDA receptor negative allosteric modulator at the same binding site as phencyclidine.[22] Amitriptyline inhibits sodium channels, L-type calcium channels, and Kv1.1, Kv7.2, and Kv7.3 voltage-gated potassium channels, and therefore acts as a sodium, calcium, and potassium channel blocker as well.[23][24][25]
Recently, amitriptyline has been demonstrated to act as an agonist of the TrkA and TrkB receptors.[26] It promotes the heterodimerization of these proteins in the absence of NGF and has potent neurotrophic activity both in-vivo and in-vitro in mouse models.[26][27] These are the same receptors BDNF activate, an endogenous neurotrophin with powerful antidepressant effects, and as such this property may contribute significantly to its therapeutic efficacy against depression. Amitriptyline does also act as FIASMA (functional inhibitor of acid sphingomyelinase).[28]
History
Amitriptyline, under the brand name Elavil, was developed by Merck and approved by the FDA on April 7, 1961, for the treatment of major depression in the United States.[29] In India, Merck & Co launched amitriptyline under the brand name Tryptomer, which is now with Merind, a division of Wockhardt.
See also
References
- ^ Barbui C, Hotopf M (February 2001). "Amitriptyline v. the rest: still the leading antidepressant after 40 years of randomised controlled trials". The British Journal of Psychiatry : the Journal of Mental Science 178 (2): 129–144. doi:10.1192/bjp.178.2.129. PMID 11157426. http://bjp.rcpsych.org/cgi/pmidlookup?view=long&pmid=11157426.
- ^ "Amitriptyline Hydrochloride". The American Society of Health-System Pharmacists. http://www.drugs.com/monograph/amitriptyline-hydrochloride.html. Retrieved 3 April 2011.
- ^ S. G. Hubscher et al. (2006). Functional biliary type pain syndrome. In P. J. Pasricha, W. D. Willis & G. F. Gebhart (Eds.), ' ' italics' ' Chronic Abdominal and Visceral Pain' 'italics' '. London: Informa Healthcare, pp. 459-461.
- ^ http://www.patient.co.uk/health/Bedwetting-Medicine-Treatments.htm
- ^ National Institute for Clinical Excellence: The Treatment of PTSD in Adults and Children
- ^ British National Formulary 45 (March 2003).
- ^ Otaka M, Jin M, Odashima M et al. (June 2005). "New strategy of therapy for functional dyspepsia using famotidine, mosapride and amitriptyline". Aliment. Pharmacol. Ther. 21 (Suppl 2): 42–46. doi:10.1111/j.1365-2036.2005.02473.x. PMID 15943846. http://www.ingentaconnect.com/content/bsc/apt/2005/00000021/A00201s2/art00008.
- ^ Healthline.com -Connect to Better Health
- ^ http://www.indydiscoverynetwork.org/AnticholinergicCognitiveBurdenScale.html
- ^ http://www.cfas.ac.uk/
- ^ Drug-induced liver disease By Neil Kaplowitz, Laurie D. DeLeve; pag.527; http://books.google.com/books?id=ecgazhSpVX8C&pg=PA528&lpg=PA528&dq=Amitriptyline+hepatotoxic&source=bl&ots=MISv72vwjy&sig=3AwKzSeTEWjbqWKzlBSqeLjABHU&hl=en&ei=6XKkTseLA8SKswaF863gAg&sa=X&oi=book_result&ct=result&resnum=1&ved=0CBoQ6AEwADgK#v=onepage&q&f=false
- ^ http://bnf.org/bnf/bnf/current/3295.htm
- ^ http://www.cnsforum.com/content/pictures/imagebank/hirespng/antidep_uptake_specific.png
- ^ a b Tatsumi; Groshan, K.; Blakely, R. D.; Richelson, E. (1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European Journal of Pharmacology 340 (2–3): 249–258. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821. edit
- ^ Albert Ellis; Gwynn Pennant Ellis (1 January 1987). Progress in Medicinal Chemistry. Elsevier. p. 56. ISBN 978-0-444-80876-9. http://books.google.com/books?id=jr0u58hFDhEC&pg=PA56. Retrieved 27 November 2011.
- ^ Nguyen T, Shapiro DA, George SR, et al. (March 2001). "Discovery of a novel member of the histamine receptor family". Molecular Pharmacology 59 (3): 427–33. PMID 11179435. http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=11179435.
- ^ D. Sriram & P. Yogeeswari (1 September 2010). Medicinal Chemistry. Pearson Education India. p. 299. ISBN 978-81-317-3144-4. http://books.google.com/books?id=tUSLclf_NoQC&pg=PA299. Retrieved 27 November 2011.
- ^ Owens; Morgan, WN; Plott, SJ; Nemeroff, CB (1997). "Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites". The Journal of Pharmacology and Experimental Therapeutics 283 (3): 1305–22. PMID 9400006. edit
- ^ Alan F. Schatzberg, Charles B. (2006). Essentials of clinical psychopharmacology. American Psychiatric Pub. p. 7. ISBN 1-58562-243-5, 9781585622436.
- ^ Rauser; Savage, J. E.; Meltzer, H. Y.; Roth, B. L. (2001). "Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor". The Journal of Pharmacology and Experimental Therapeutics 299 (1): 83–89. PMID 11561066. edit
- ^ Werling; Keller, A. .; Frank, J. .; Nuwayhid, S. . (2007). "A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder". Experimental neurology 207 (2): 248–257. doi:10.1016/j.expneurol.2007.06.013. PMID 17689532. edit
- ^ Sills; Loo, PS (1989). "Tricyclic antidepressants and dextromethorphan bind with higher affinity to the phencyclidine receptor in the absence of magnesium and L-glutamate". Molecular Pharmacology 36 (1): 160–5. PMID 2568580. edit
- ^ Pancrazio; Kamatchi, GL; Roscoe, AK; Lynch C, 3rd (1998). "Inhibition of neuronal Na+ channels by antidepressant drugs". The Journal of Pharmacology and Experimental Therapeutics 284 (1): 208–14. PMID 9435180. edit
- ^ Zahradnik, I. .; Minarovic, I. .; Zahradnikova, A. . (2008). "Inhibition of the cardiac L-type calcium channel current by antidepressant drugs". The Journal of Pharmacology and Experimental Therapeutics 324 (3): 977–984. doi:10.1124/jpet.107.132456. PMID 18048694. edit
- ^ Punke MA, Friederich P (May 2007). "Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels". Anesthesia and Analgesia 104 (5): 1256–1264. doi:10.1213/01.ane.0000260310.63117.a2. PMID 17456683. http://www.anesthesia-analgesia.org/cgi/pmidlookup?view=long&pmid=17456683.
- ^ a b Jang; Liu, X. .; Chan, C. .; Weinshenker, D. .; Hall, R. .; Xiao, G. .; Ye, K. . (2009). "Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity". Chemistry & biology 16 (6): 644–656. doi:10.1016/j.chembiol.2009.05.010. PMC 2844702. PMID 19549602. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2844702. edit
- ^ http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20(General%20Monographs-%20A)/AMITRIPTYLINE.html
- ^ Kornhuber J, Muehlbacher M, Trapp S, Pechmann S, Friedl A, Reichel M, Mühle C, Terfloth L, Groemer T, Spitzer G, Liedl K, Gulbins E, Tripal P (2011). "Identification of novel functional inhibitors of acid sphingomyelinase". PLoS ONE 6 (8): e23852. doi:10.1371/journal.pone.0023852.
- ^ Fangmann P, Assion HJ, Juckel G, González CA, López-Muñoz F (February 2008). "Half a century of antidepressant drugs: on the clinical introduction of monoamine oxidase inhibitors, tricyclics, and tetracyclics. Part II: tricyclics and tetracyclics". Journal of Clinical Psychopharmacology 28 (1): 1–4. doi:10.1097/jcp.0b013e3181627b60. PMID 18204333. http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0271-0749&volume=28&issue=1&spage=1.
Further reading
- PubChem Substance Summary: Amitriptyline National Center for Biotechnology Information.
- TREPILINE-10 TABLETS; TREPILINE-25 TABLETS South African Electronic Package Inserts. 12 May 1978. Revised February 2004.
- SAROTEN RETARD 25 mg Capsules; SAROTEN RETARD 50 mg Capsules South African Electronic Package Inserts. December 1987. Updated May 2000.
- AMITRIP Amitriptyline hydrochloride 10 mg, 25 mg and 50 mg Capsules Medsafe NZ Physician Data Sheet. November 2004.
- Endep Consumer Medicine Information, Australia. December 2005.
- MedlinePlus Drug Information: Amitriptyline. US National Institutes of Health. January 2008.
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Antidepressants (N06A)
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Specific reuptake inhibitors (RIs), enhancers (REs), and releasing agents (RAs)
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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dsrd (o, p, m, p, a, d, s), sysi/epon, spvo
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| H1 Antagonists |
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| Others |
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- WAY-267,464
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|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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dsrd (o, p, m, p, a, d, s), sysi/epon, spvo
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proc(eval/thrp), drug(N5A/5B/5C/6A/6B/6D)
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Hypnotics/sedatives (N05C)
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Carbamates: Carisoprodol • Ethinamate • Hexapropymate • Meprobamate • Methocarbamol • Procymate • Tybamate
Neuroactive Steroids: Acebrochol • Allopregnanolone • Alphadolone • Alphaxolone • Eltanolone • Ganaxolone • Hydroxydione • Minaxolone • Org 20599 • Org 21465 • Tetrahydrodeoxycorticosterone
Nonbenzodiazepines: CL-218,872 • Eszopiclone • Indiplon • JM-1232 • Lirequinil • Necopidem • Pazinaclone • ROD-188 • Saripidem • Suproclone • Suriclone • SX-3228 • U-89843A • U-90042 • Zaleplon • Zolpidem • Zopiclone
Phenols: Fospropofol • Propofol
Piperidinediones: Glutethimide • Methyprylon • Pyrithyldione • Piperidione
Quinazolinones: Afloqualone • Cloroqualone • Diproqualone • Etaqualone • Mebroqualone • Mecloqualone • Methaqualone • Methylmethaqualone • Nitromethaqualone • SL-164
Volatiles/gases: 2-Methyl-2-butanol • Acetophenone • Acetylglycinamide chloral hydrate • Centalun • Chloral hydrate • Ethanol (Alcohol) • Paraldehyde • Trichloroethanol
Others: Bromide (Lithium bromide, Potassium bromide, Sodium bromide) • Chloralose • Chloralodol • Clomethiazole • Dichloralphenazone • Ethchlorvynol • Etomidate • Gaboxadol • Loreclezole • Methylpentynol • Metomidate • Org 25435 • Petrichloral • Sulfonmethane • Triclofos • Valerenic acid (Valerian)
|
|
| GABAB agonists |
1,4-Butanediol • Aceburic acid • GABOB • GHB (Sodium oxybate) • GBL • GVL
|
|
| H1 inverse agonists |
Antihistamines: Captodiame • Cyproheptadine • Diphenhydramine • Doxylamine • Hydroxyzine • Methapyrilene • Pheniramine • Promethazine • Propiomazine
Antidepressants: Tricyclic antidepressants (Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
|
|
| α1-Adrenergic antagonists |
Antidepressants: Serotonin antagonists and reuptake inhibitors (Trazodone) • Tricyclic antidepressants ( Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
Others: Niaprazine
|
|
| α2-Adrenergic agonists |
4-NEMD • Clonidine • Detomidine • Dexmedetomidine • Lofexidine • Medetomidine • Romifidine • Tizanidine • Xylazine
|
|
| 5-HT2A antagonists |
Antidepressants: Serotonin antagonists and reuptake inhibitors (Trazodone) • Tricyclic antidepressants ( Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
Others: Eplivanserin • Niaprazine • Pruvanserin • Volinanserin
|
|
| Melatonin agonists |
Agomelatine • LY-156,735 • Melatonin • Ramelteon • Tasimelteon
|
|
| Orexin antagonists |
Almorexant • SB-334,867 • SB-408,124 • SB-649,868 • Suvorexant • TCS-OX2-29
|
|
| Others |
Acecarbromal • Apronal • Bromisoval • Cannabidiol (Cannabis) • Carbromal • Embutramide • Evoxine • Fenadiazole • Gabapentin • Kavalactones (Kava) • Mephenoxalone • Opioids (Oxycodone, Morphine (Opium), etc.) • Passion flower • Scopolamine (Mandrake) • Valnoctamide
|
|
|
Orexigenics (A15)
|
|
| Exogenous |
- Amitriptyline
- Clonidine
- Cyproheptadine
- Dexamethasone
- Dronabinol/Tetrahydrocannabinol (Cannabis)
- Medroxyprogesterone acetate
- Megestrol acetate
- Mirtazapine
- Nabilone
- Nandrolone
- Olanzapine
- Omega-3 fatty acids
- Oxandrolone
- Pentoxifylline
- Prednisone
- Sugars
- Testosterone
- Thalidomide
|
|
| Endogenous |
- ACTH/Corticotropin
- Adiponectin
- Agouti-related peptide
- Anandamide
- Cortisol/Hydrocortisone
- Cortisone
- Ghrelin
- Melanin-concentrating hormone
- Melatonin
- Neuropeptide Y
- Orexin/Hypocretin
|
|
|
Adrenergics
|
|
|
Receptor ligands
|
|
|
α1
|
- Agonists: 5-FNE
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Cirazoline
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Indanidine
- Levonordefrin
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- CI-926
- Corynanthine
- Dapiprazole
- DL-017
- Domesticine
- Doxazosin
- Eugenodilol
- Fenspiride
- GYKI-12,743
- GYKI-16,084
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- Mephendioxan
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Neldazosin
- Nicergoline
- Niguldipine
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- RS-97,078
- SGB-1,534
- Silodosin
- SL-89.0591
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazoline
- Trimazosin
- Upidosin
- Urapidil
- Zolertine
* Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone and trazodone all antagonize α1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
|
|
|
α2
|
- Agonists: (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Ephedrine
- Ergotamine
- Epinephrine
- Esproquin
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- Levonordefrin
- Lofexidine
- Medetomidine
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tizanidine
- Tolonidine
- Urapidil
- Xylazine
- Xylometazoline
Antagonists: 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- GYKI-12,743
- GYKI-16,084
- Idazoxan
- Mianserin
- Mirtazapine
- MK-912
- NAN-190
- Olanzapine
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269,970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Yohimbine
* Note that many atypical antipsychotics and azapirones like buspirone (via metabolite 1-PP) antagonize α2-adrenergic receptors as well.
|
|
|
β
|
|
|
|
|
|
Reuptake inhibitors
|
|
|
NET
|
- Selective norepinephrine reuptake inhibitors: Amedalin
- Atomoxetine (Tomoxetine)
- Ciclazindol
- Daledalin
- Edivoxetine
- Esreboxetine
- Lortalamine
- Mazindol
- Nisoxetine
- Reboxetine
- Talopram
- Talsupram
- Tandamine
- Viloxazine; Norepinephrine-dopamine reuptake inhibitors: Amineptine
- Bupropion (Amfebutamone)
- Fencamine
- Fencamfamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Methylphenidate
- Nomifensine
- O-2172
- Radafaxine; Serotonin-norepinephrine reuptake inhibitors: Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- Sibutramine
- Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- JNJ-7925476
- JZ-IV-10
- Methylnaphthidate
- Naphyrone
- NS-2359
- PRC200-SS
- SEP-225,289
- SEP-227,162
- Tesofensine; Tricyclic antidepressants: Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- melitracen
- Nortriptyline
- Protriptyline
- Trimipramine; Tetracyclic antidepressants: Amoxapine
- Maprotiline
- Mianserin
- Oxaprotiline
- Setiptiline; Others: Cocaine
- CP-39,332
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Nefopam
- Pridefrine
- Tapentadol
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tramadol
- Ziprasidone
|
|
|
VMAT
|
- Ibogaine
- Reserpine
- Tetrabenazine
|
|
|
|
|
|
|
|
Enzyme inhibitors
|
|
|
Anabolism
|
|
PAH
|
|
|
|
TH
|
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
|
|
|
AAAD
|
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
|
|
|
DBH
|
- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
|
|
|
PNMT
|
- CGS-19281A
- SKF-64139
- SKF-7698
|
|
|
|
Catabolism
|
|
MAO
|
- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Befol
- Brofaromine
- Cimoxatone
- Clorgiline
- Esuprone
- Harmala alkaloids (Harmine,
- Harmaline
- Tetrahydroharmine
- Harman
- Norharman, etc)
- Methylene blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective:
- Ladostigil
- Lazabemide
- Milacemide
- Mofegiline
- Pargyline
- Rasagiline
- Safinamide
- Selegiline (also [[D-Deprenyl]])
* Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.
|
|
|
COMT
|
- Entacapone
- Nitecapone
- Tolcapone
|
|
|
|
|
|
Others
|
|
|
Precursors
|
- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
|
|
|
Cofactors
|
- Ferrous Iron (Fe2+)
- S-Adenosyl-L-Methionine
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal Phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
|
|
|
Others
|
- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
|
|
|
|
|
List of adrenergic drugs
|
|
|
Cholinergics
|
|
|
Receptor ligands
|
|
|
mAChR
|
- Agonists: 77-LH-28-1
- AC-42
- AC-260,584
- Aceclidine
- Acetylcholine
- AF30
- AF150(S)
- AF267B
- AFDX-384
- Alvameline
- AQRA-741
- Arecoline
- Bethanechol
- Butyrylcholine
- Carbachol
- CDD-0034
- CDD-0078
- CDD-0097
- CDD-0098
- CDD-0102
- Cevimeline
- Choline
- cis-Dioxolane
- Ethoxysebacylcholine
- LY-593,039
- L-689,660
- LY-2,033,298
- McNA343
- Methacholine
- Milameline
- Muscarine
- NGX-267
- Ocvimeline
- Oxotremorine
- PD-151,832
- Pilocarpine
- RS86
- Sabcomeline
- SDZ 210-086
- Sebacylcholine
- Suberylcholine
- Talsaclidine
- Tazomeline
- Thiopilocarpine
- Vedaclidine
- VU-0029767
- VU-0090157
- VU-0152099
- VU-0152100
- VU-0238429
- WAY-132,983
- Xanomeline
- YM-796
Antagonists: 3-Quinuclidinyl Benzilate
- 4-DAMP
- Aclidinium Bromide
- Anisodamine
- Anisodine
- Atropine
- Atropine Methonitrate
- Benactyzine
- Benzatropine/Benztropine
- Benzydamine
- BIBN 99
- Biperiden
- Bornaprine
- CAR-226,086
- CAR-301,060
- CAR-302,196
- CAR-302,282
- CAR-302,368
- CAR-302,537
- CAR-302,668
- CS-27349
- Cyclobenzaprine
- Cyclopentolate
- Darifenacin
- DAU-5884
- Dimethindene
- Dexetimide
- DIBD
- Dicyclomine/Dicycloverine
- Ditran
- EA-3167
- EA-3443
- EA-3580
- EA-3834
- Etanautine
- Etybenzatropine/Ethylbenztropine
- Flavoxate
- Himbacine
- HL-031,120
- Ipratropium bromide
- J-104,129
- Hyoscyamine
- Mamba Toxin 3
- Mamba Toxin 7
- Mazaticol
- Mebeverine
- Methoctramine
- Metixene
- N-Ethyl-3-Piperidyl Benzilate
- N-Methyl-3-Piperidyl Benzilate
- Orphenadrine
- Otenzepad
- Oxybutynin
- PBID
- PD-102,807
- PD-0298029
- Phenglutarimide
- Phenyltoloxamine
- Pirenzepine
- Piroheptine
- Procyclidine
- Profenamine
- RU-47,213
- SCH-57,790
- SCH-72,788
- SCH-217,443
- Scopolamine/Hyoscine
- Solifenacin
- Telenzepine
- Tiotropium bromide
- Tolterodine
- Trihexyphenidyl
- Tripitamine
- Tropatepine
- Tropicamide
- WIN-2299
- Xanomeline
- Zamifenacin; Others: 1st Generation Antihistamines (Brompheniramine
- chlorphenamine
- cyproheptadine
- dimenhydrinate
- diphenhydramine
- doxylamine
- mepyramine/pyrilamine
- phenindamine
- pheniramine
- tripelennamine
- triprolidine, etc)
- Tricyclic Antidepressants (Amitriptyline
- doxepin
- trimipramine, etc)
- Tetracyclic Antidepressants (Amoxapine
- maprotiline, etc)
- Typical Antipsychotics (Chlorpromazine
- thioridazine, etc)
- Atypical Antipsychotics (Clozapine
- olanzapine
- quetiapine, etc)
|
|
|
nAChR
|
- Agonists: 5-HIAA
- A-84,543
- A-366,833
- A-582,941
- A-867,744
- ABT-202
- ABT-418
- ABT-560
- ABT-894
- Acetylcholine
- Altinicline
- Anabasine
- Anatoxin-a
- AR-R17779
- Butinoline
- Butyrylcholine
- Carbachol
- Choline
- Cotinine
- Cytisine
- Decamethonium
- Desformylflustrabromine
- Dianicline
- Dimethylphenylpiperazinium
- Epibatidine
- Epiboxidine
- Ethanol
- Ethoxysebacylcholine
- EVP-4473
- EVP-6124
- Galantamine
- GTS-21
- Ispronicline
- Lobeline
- MEM-63,908/RG-3487
- Nicotine
- NS-1738
- PHA-543,613
- PHA-709,829
- PNU-120,596
- PNU-282,987
- Pozanicline
- Rivanicline
- RJR-2429
- Sazetidine A
- Sebacylcholine
- SIB-1508Y
- SIB-1553A
- SSR-180,711
- Suberylcholine
- TC-1698
- TC-1734
- TC-1827
- TC-2216
- TC-5214
- TC-5619
- TC-6683
- Tebanicline
- Tropisetron
- UB-165
- Varenicline
- WAY-317,538
- XY-4083
Antagonists: 18-Methoxycoronaridine
- α-Bungarotoxin
- α-Conotoxin
- Alcuronium
- Amantadine
- Anatruxonium
- Atracurium
- Bupropion
- Chandonium
- Chlorisondamine
- Cisatracurium
- Coclaurine
- Coronaridine
- Dacuronium
- Decamethonium
- Dextromethorphan
- Dextropropoxyphene
- Dextrorphan
- Diadonium
- DHβE
- Dimethyltubocurarine/Metocurine
- Dipyrandium
- Dizocilpine/MK-801
- Doxacurium
- Duador
- Esketamine
- Fazadinium
- Gallamine
- Hexafluronium
- Hexamethonium/Benzohexonium
- Ibogaine
- Isoflurane
- Ketamine
- Kynurenic acid
- Laudexium/Laudolissin
- Levacetylmethadol
- Malouetine
- Mecamylamine
- Memantine
- Methadone (Levomethadone)
- Methorphan/Racemethorphan
- Methyllycaconitine
- Metocurine
- Mivacurium
- Morphanol/Racemorphan
- Neramexane
- Nitrous Oxide
- Pancuronium
- Pempidine
- Pentamine
- Pentolinium
- Phencyclidine
- Pipecuronium
- Radafaxine
- Rapacuronium
- Rocuronium
- Surugatoxin
- Suxamethonium/Succinylcholine
- Thiocolchicoside
- Toxiferine
- Trimethaphan
- Tropeinium
- Tubocurarine
- Vecuronium
- Xenon
|
|
|
|
|
Reuptake inhibitors
|
|
|
Plasmalemmal
|
|
CHT Inhibitors
|
- Hemicholinium-3/Hemicholine
- Triethylcholine
|
|
|
|
Vesicular
|
|
|
|
|
|
Enzyme inhibitors
|
|
|
Anabolism
|
|
ChAT inhibitors
|
- 1-(-Benzoylethyl)pyridinium
- 2-(α-Naphthoyl)ethyltrimethylammonium
- 3-Chloro-4-stillbazole
- 4-(1-Naphthylvinyl)pyridine
- Acetylseco hemicholinium-3
- Acryloylcholine
- AF64A
- B115
- BETA
- CM-54,903
- N,N-Dimethylaminoethylacrylate
- N,N-Dimethylaminoethylchloroacetate
|
|
|
|
Catabolism
|
|
AChE inhibitors
|
|
|
|
BChE inhibitors
|
- Cymserine * Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.
|
|
|
|
|
|
Others
|
|
|
Precursors
|
- Choline (Lecithin)
- Citicoline
- Cyprodenate
- Dimethylethanolamine
- Glycerophosphocholine
- Meclofenoxate/Centrophenoxine
- Phosphatidylcholine
- Phosphatidylethanolamine
- Phosphorylcholine
- Pirisudanol
|
|
|
Cofactors
|
- Acetic acid
- Acetylcarnitine
- Acetyl-coA
- Vitamin B5 (Pantethine
- Pantetheine
- Panthenol)
|
|
|
Others
|
- Acetylcholine releasing agents: α-Latrotoxin
- β-Bungarotoxin; Acetylcholine release inhibitors: Botulinum toxin (Botox); Acetylcholinesterase reactivators: Asoxime
- Obidoxime
- Pralidoxime
|
|
|
|
|
Glutamatergics
|
|
| Ionotropic |
|
AMPA
|
- Agonists: 5-Fluorowillardiine
- AMPA
- Domoic acid
- Quisqualic acid; Positive allosteric modulators: Aniracetam
- Cyclothiazide
- CX-516
- CX-546
- CX-614
- CX-691
- CX-717
- Diazoxide
- HCTZ
- IDRA-21
- LY-392,098
- LY-404,187
- LY-451,395
- LY-451,646
- LY-503,430
- Org 26576
- Oxiracetam
- PEPA
- Piracetam
- Pramiracetam
- S-18986
- Sunifiram
- Unifiram
Antagonists: ATPO
- Barbiturates
- BGG492
- Caroverine
- CNQX
- DNQX
- GYKI-52466
- NBQX
- Perampanel
- Talampanel
- Tezampanel
- Topiramate; Negative allosteric modulators: GYKI-53,655
|
|
|
NMDA
|
- Agonists: Glutamate/acite site competitive agonists: Aspartate
- Glutamate
- Homoquinolinic acid
- Ibotenic acid
- NMDA
- Quinolinic acid
- Tetrazolylglycine; Glycine site agonists: ACBD
- ACPC
- ACPD
- Alanine
- CCG
- Cycloserine
- DHPG
- Fluoroalanine
- Glycine
- HA-966
- L-687,414
- Milacemide
- Sarcosine
- Serine
- Tetrazolylglycine; Polyamine site agonists: Acamprosate
- Spermidine
- Spermine
Antagonists: Competitive antagonists: AP5 (APV)
- AP7
- CGP-37849
- CGP-39551
- CGP-39653
- CGP-40116
- CGS-19755
- CPP
- LY-233,053
- LY-235,959
- LY-274,614
- MDL-100,453
- Midafotel (d-CPPene)
- NPC-12,626
- NPC-17,742
- PBPD
- PEAQX
- Perzinfotel
- PPDA
- SDZ-220581
- Selfotel; Noncompetitive antagonists: ARR-15,896
- Caroverine
- Dexanabinol
- FPL-12495
- FR-115,427
- Hodgkinsine
- Magnesium
- MDL-27,266
- NPS-1506
- Psychotridine
- Zinc; Uncompetitive pore blockers: 2-MDP
- 3-MeO-PCP
- 8A-PDHQ
- Alaproclate
- Amantadine
- Aptiganel
- ARL-12,495
- ARL-15,896-AR
- ARL-16,247
- Budipine
- Delucemine
- Dexoxadrol
- Dextrallorphan
- Dieticyclidine
- Dizocilpine
- Endopsychosin
- Esketamine
- Etoxadrol
- Eticyclidine
- Gacyclidine
- Ibogaine
- Indantadol
- Ketamine
- Ketobemidone
- Loperamide
- Memantine
- Meperidine (Pethidine)
- Methadone (Levomethadone)
- Methorphan (Dextromethorphan
- Levomethorphan)
- Methoxetamine
- Milnacipran
- Morphanol (Dextrorphan
- Levorphanol)
- NEFA
- Neramexane
- Nitrous oxide
- Noribogaine
- Orphenadrine
- PCPr
- Phencyclamine
- Phencyclidine
- Propoxyphene
- Remacemide
- Rhynchophylline
- Riluzole
- Rimantadine
- Rolicyclidine
- Sabeluzole
- Tenocyclidine
- Tiletamine
- Tramadol
- Xenon; Glycine site antagonists: ACEA-1021
- ACEA-1328
- ACPC
- Carisoprodol
- CGP-39653
- CKA
- DCKA
- Felbamate
- Gavestinel
- GV-196,771
- Kynurenic acid
- L-689,560
- L-701,324
- Lacosamide
- Licostinel
- LU-73,068
- MDL-105,519
- Meprobamate
- MRZ 2/576
- PNQX
- ZD-9379; NR2B subunit antagonists: Besonprodil
- CO-101,244 (PD-174,494)
- CP-101,606
- Eliprodil
- Haloperidol
- Ifenprodil
- Isoxsuprine
- Nylidrin
- Ro8-4304
- Ro25-6981
- Traxoprodil; Polyamine site antagonists: Arcaine
- Co 101676
- Diaminopropane
- Acamprosate
- Diethylenetriamine
- Huperzine A
- Putrescine
- Ro 25-6981; Unclassified/unsorted antagonists: Chloroform
- Diethyl ether
- Enflurane
- Ethanol (Alcohol)
- Halothane
- Isoflurane
- Methoxyflurane
- Toluene
- Trichloroethane
- Trichloroethanol
- Trichloroethylene
- Xylene
|
|
|
Kainate
|
- Agonists: 5-Iodowillardiine
- ATPA
- Domoic acid
- Kainic acid
- LY-339,434
- SYM-2081
Antagonists: BGG492
- CNQX
- DNQX
- LY-382,884
- NBQX
- NS102
- Tezampanel
- Topiramate
- UBP-302; Negative allosteric modulators: NS-3763
|
|
|
| Metabotropic |
|
Group I
|
- Agonists: Non-selective: ACPD
- DHPG
- Quisqualic acid; mGlu1-selective: Ro01-6128
- Ro67-4853
- Ro67-7476
- VU-71; mGlu5-selective: ADX-47273
- CDPPB
- CHPG
- DFB
- VU-1545
Antagonists: Non-selective: MCPG
- NPS-2390; mGlu1-selective: BAY 36-7620
- CPCCOEt
- LY-367,385
- LY-456,236; mGlu5-selective: CTEP
- Dipraglurant
- DMeOB
- LY-344,545
- SIB-1757
- SIB-1893; Negative allosteric modulators: Fenobam
- MPEP
- MTEP
- GRN-529
|
|
|
Group II
|
- Agonists: Non-selective: CBiPES
- DCG-IV
- Eglumegad
- LY-379,268
- LY-404,039
- LY-487,379
- MGS-0028; mGlu2-selective: BINA
- LY-566,332
Antagonists: Non-selective: APICA
- EGLU
- HYDIA
- LY-307,452
- LY-341,495
- MCPG
- MGS-0039: mGlu2-selective: PCCG-4; mGlu3-selective: CECXG; Negative allosteric modulators: RO4491533
|
|
|
Group III
|
- Agonists: Non-selective: L-AP4; mGlu4-selective: PHCCC
- VU-001,171
- VU-0155,041; mGlu7-selective: AMN082; mGlu8-selective: DCPG
Antagonists: Non-selective: CPPG
- MAP4
- MSOP
- MPPG
- MTPG
- UBP-1112; mGlu7-selective: MMPIP
|
|
|
Transporter
inhibitors |
|
|
| Others |
|
Precursors
|
|
|
|
Cofactors
|
- α-Ketoglutaric acid
- Iron
- Sulfur
- Vitamin B2 (as FAD and FMN)
- Vitamin B3 (as NADPH)
|
|
|
Others
|
|
|
|
|
Histaminergics
|
|
| Receptor |
|
H1
|
- Agonists: 2-Pyridylethylamine
- Betahistine
- Histamine
- HTMT
- UR-AK49
Antagonists: 1st generation: 4-Methyldiphenhydramine
- Alimemazine
- Antazoline
- Azatadine
- Bamipine
- Benzatropine/Benztropine
- Bepotastine
- Bromazine
- Brompheniramine
- Buclizine
- Captodiame
- Carbinoxamine
- Chlorcyclizine
- Chloropyramine
- Chlorothen
- Chlorphenamine
- Chlorphenoxamine
- Cinnarizine
- Clemastine
- Clobenzepam
- Clocinizine
- Cyclizine
- Cyproheptadine
- Dacemazine
- Deptropine
- Dexbrompheniramine
- Dexchlorpheniramine
- Dimenhydrinate
- Dimetindene
- Diphenhydramine
- Diphenylpyraline
- Doxylamine
- Embramine
- Etodroxizine
- Etybenzatropine/Ethylbenztropine
- Etymemazine
- Flunarizine
- Histapyrrodine
- Homochlorcyclizine
- Hydroxyethylpromethazine
- Hydroxyzine
- Isopromethazine
- Isothipendyl
- Meclozine
- Mepyramine/Pyrilamine
- Mequitazine
- Methafurylene
- Methapyrilene
- Methdilazine
- Moxastine
- Niaprazine
- Orphenadrine
- Oxatomide
- Oxomemazine
- Phenindamine
- Pheniramine
- Phenyltoloxamine
- Pimethixene
- Piperoxan
- Pipoxizine
- Promethazine
- Propiomazine
- Pyrrobutamine
- Talastine
- Thenalidine
- Thenyldiamine
- Thiazinamium
- Thonzylamine
- Tolpropamine
- Tripelennamine
- Triprolidine
- 2nd generation: Acrivastine
- Alinastine
- Astemizole
- Azelastine
- Bamirastine
- Barmastine
- Bepiastine
- Bepotastine
- Bilastine
- Cabastinen
- Carebastine
- Cetirizine
- Clemastine
- Clemizole
- Clobenztropine
- Dorastine
- Ebastine
- Emedastine
- Epinastine
- Flezelastine
- Ketotifen
- Latrepirdine
- Levocabastine
- Linetastine
- Loratadine
- Mapinastine
- Mebhydrolin
- Mizolastine
- Moxastine
- Noberastine
- Octastine
- Olopatadine
- Perastine
- Piclopastine
- Rocastine
- Rupatadine
- Setastine
- Talastine
- Temelastine
- Terfenadine
- Zepastine
- 3rd generation: Desloratadine
- Fexofenadine
- Levocetirizine
- Ungrouped: Belarizine
- Efletirizine
- Elbanizine
- Flotrenizine
- Medrylamine
- Napactadine
- Pibaxizine
- Tagorizine
- Trelnarizine
- Trenizine
- Vapitadine
- Miscellaneous: Tricyclic antidepressants (amitriptyline,
- doxepin,
- trimipramine, etc)
- Tetracyclic antidepressants (mianserin,
- mirtazapine, etc)
- Typical antipsychotics (chlorpromazine,
- thioridazine, etc)
- Atypical antipsychotics (clozapine,
- olanzapine,
- quetiapine, etc)
|
|
|
H2
|
- Agonists: Amthamine
- Betazole
- Dimaprit
- Histamine
- HTMT
- Impromidine
- UR-AK49
Antagonists: Bisfentidine
- Burimamide
- Cimetidine
- Dalcotidine
- Donetidine
- Ebrotidine
- Etintidine
- Famotidine
- Lafutidine
- Lamtidine
- Lavoltidine/Loxtidine
- Lupitidine
- Metiamide
- Mifentidine
- Niperotidine
- Nizatidine
- Osutidine
- Oxmetidine
- Pibutidine
- Quisultazine/Quisultidine
- Ramixotidine
- Ranitidine
- Roxatidine
- Sufotidine
- Tiotidine
- Tuvatidine
- Venritidine
- Xaltidine
|
|
|
H3
|
- Agonists: α-Methylhistamine
- Cipralisant
- Histamine
- Imetit
- Immepip
- Immethridine
- Methimepip
- Proxyfan
Antagonists: A-349,821
- A-423,579
- ABT-239
- Betahistine
- Burimamide
- Ciproxifan
- Clobenpropit
- Conessine
- GSK-189,254
- Impentamine
- Iodophenpropit
- JNJ-5,207,852
- MK-0249
- NNC-38-1,049
- PF-03654746
- Pitolisant
- SCH-79,687
- Thioperamide
- VUF-5,681
|
|
|
H4
|
- Agonists: 4-Methylhistamine
- Histamine
- VUF-8,430
Antagonists: JNJ-7,777,120
- Thioperamide
- VUF-6,002
|
|
|
| Transporter |
|
VMAT
|
- Inhibitors: Ibogaine
- Reserpine
- Tetrabenazine
|
|
|
| Enzyme |
|
HDC
|
- Inhibitors: Catechin
- Meciadanol
- Naringenin
- Tritoqualine
|
|
|
DAO
|
- Inhibitors: Aminoguanidine
|
|
|
| Others |
|
Endogenous
|
- Histamine; Precursors: L-Histidine; Cofactors: Vitamin B6
|
|
|
|
Serotonergics
|
|
|
5-HT1 receptor ligands
|
|
|
5-HT1A
|
- Agonists: Azapirones: Alnespirone
- Binospirone
- Buspirone
- Enilospirone
- Eptapirone
- Gepirone
- Ipsapirone
- Perospirone
- Revospirone
- Tandospirone
- Tiospirone
- Umespirone
- Zalospirone; Antidepressants: Etoperidone
- Nefazodone
- Trazodone
- Vortioxetine; Antipsychotics: Aripiprazole
- Asenapine
- Clozapine
- Quetiapine
- Ziprasidone; Ergolines: Dihydroergotamine
- Ergotamine
- Lisuride
- Methysergide
- LSD; Tryptamines: 5-CT
- 5-MeO-DMT
- 5-MT
- Bufotenin
- DMT
- Indorenate
- Psilocin
- Psilocybin; Others: 8-OH-DPAT
- Adatanserin
- Bay R 1531
- Befiradol
- BMY-14802
- Cannabidiol
- Dimemebfe
- Ebalzotan
- Eltoprazine
- F-11,461
- F-12,826
- F-13,714
- F-14,679
- F-15,063
- F-15,599
- Flesinoxan
- Flibanserin
- Lesopitron
- LY-293,284
- LY-301,317
- MKC-242
- Naluzotan
- NBUMP
- Osemozotan
- Oxaflozane
- Pardoprunox
- Piclozotan
- Rauwolscine
- Repinotan
- Roxindole
- RU-24,969
- S 14,506
- S-14,671
- S-15,535
- Sarizotan
- SSR-181,507
- Sunepitron
- U-92,016-A
- Urapidil
- Vilazodone
- Xaliproden
- Yohimbine
Antagonists: Antipsychotics: Iloperidone
- Risperidone
- Sertindole; Beta blockers: Alprenolol
- Cyanopindolol
- Iodocyanopindolol
- Oxprenolol
- Pindobind
- Pindolol
- Propranolol
- Tertatolol; Others: AV965
- BMY-7,378
- CSP-2503
- Dotarizine
- Flopropione
- GR-46611
- Isamoltane
- Lecozotan
- Mefway
- Metitepine/Methiothepin
- MPPF
- NAN-190
- Robalzotan
- S-15535
- SB-649,915
- SDZ 216-525
- Spiperone
- Spiramide
- Spiroxatrine
- UH-301
- WAY-100,135
- WAY-100,635
- Xylamidine
|
|
|
5-HT1B
|
- Agonists: Lysergamides: Dihydroergotamine
- Ergotamine
- Methysergide; Piperazines: Eltoprazine
- TFMPP; Triptans: Avitriptan
- Eletriptan
- Sumatriptan
- Zolmitriptan; Tryptamines: 5-CT
- 5-MT; Others: CGS-12066A
- CP-93,129
- CP-94,253
- CP-135,807
- RU-24,969
- Vortioxetine
Antagonists: Lysergamides: Metergoline; Others: AR-A000002
- Elzasonan
- GR-127,935
- Isamoltane
- Metitepine/Methiothepin
- SB-216,641
- SB-224,289
- SB-236,057
- Yohimbine
|
|
|
5-HT1D
|
- Agonists: Lysergamides: Dihydroergotamine
- Methysergide; Triptans: Almotriptan
- Avitriptan
- Eletriptan
- Frovatriptan
- Naratriptan
- Rizatriptan
- Sumatriptan
- Zolmitriptan; Tryptamines: 5-CT
- 5-Ethyl-DMT
- 5-MT
- 5-(Nonyloxy)tryptamine; Others: CP-135,807
- CP-286,601
- GR-46611
- L-694,247
- L-772,405
- PNU-109,291
- PNU-142633
Antagonists: Lysergamides: Metergoline; Others: Alniditan
- BRL-15,572
- Elzasonan
- GR-127,935
- Ketanserin
- LY-310,762
- LY-367,642
- LY-456,219
- LY-456,220
- Metitepine/Methiothepin
- Ritanserin
- Yohimbine
- Ziprasidone
|
|
|
5-HT1E
|
- Agonists: Lysergamides: Methysergide; Triptans: Eletriptan; Tryptamines: BRL-54443
- Tryptamine
Antagonists: Metitepine/Methiothepin
|
|
|
5-HT1F
|
- Agonists: Triptans: Eletriptan
- Naratriptan
- Sumatriptan; Tryptamines: 5-MT; Others: BRL-54443
- Lasmiditan
- LY-334,370
Antagonists: Metitepine/Methiothepin
|
|
|
|
|
5-HT2 receptor ligands
|
|
|
|
5-HT2A
|
|
|
|
5-HT2B
|
- Agonists: Oxazolines: 4-Methylaminorex
- Aminorex; Phenethylamines: Chlorphentermine
- Cloforex
- DOB
- DOC
- DOI
- DOM
- Fenfluramine (Dexfenfluramine, Levofenfluramine)
- MDA
- MDMA
- Norfenfluramine; Tryptamines: 5-CT
- 5-MT
- α-Methyl-5-HT; Others: BW-723C86
- Cabergoline
- mCPP
- Pergolide
- PNU-22394
- Ro60-0175
Antagonists: Agomelatine
- Asenapine
- EGIS-7625
- Ketanserin
- Lisuride
- LY-272,015
- Metitepine/Methiothepin
- PRX-08066
- Rauwolscine
- Ritanserin
- RS-127,445
- Sarpogrelate
- SB-200,646
- SB-204,741
- SB-206,553
- SB-215,505
- SB-221,284
- SB-228,357
- SDZ SER-082
- Tegaserod
- Yohimbine
|
|
|
5-HT2C
|
- Agonists: Phenethylamines: 2C-B
- 2C-E
- 2C-I
- 2C-T-2
- 2C-T-7
- 2C-T-21
- DOB
- DOC
- DOI
- DOM
- MDA
- MDMA
- Mescaline; Piperazines: Aripiprazole
- mCPP
- TFMPP; Tryptamines: 5-CT
- 5-MeO-α-ET
- 5-MeO-α-MT
- 5-MeO-DET
- 5-MeO-DiPT
- 5-MeO-DMT
- 5-MeO-DPT
- 5-MT
- α-ET
- α-Methyl-5-HT
- α-MT
- Bufotenin
- DET
- DiPT
- DMT
- DPT
- Psilocin
- Psilocybin; Others: A-372,159
- AL-38022A
- CP-809,101
- Dimemebfe
- Lorcaserin
- Medifoxamine
- MK-212
- Org 12,962
- ORG-37,684
- Oxaflozane
- PNU-22394
- Ro60-0175
- Ro60-0213
- Vabicaserin
- WAY-629
- WAY-161,503
- YM-348
Antagonists: Atypical antipsychotics: Clorotepine
- Clozapine
- Iloperidone
- Melperone
- Olanzapine
- Paliperidone
- Pimozide
- Quetiapine
- Risperidone
- Sertindole
- Ziprasidone
- Zotepine; Typical antipsychotics: Chlorpromazine
- Loxapine
- Pipamperone; Antidepressants: Agomelatine
- Amitriptyline
- Amoxapine
- Aptazapine
- Etoperidone
- Fluoxetine
- Mianserin
- Mirtazapine
- Nefazodone
- Nortriptyline
- Tedatioxetine
- Trazodone; Others: Adatanserin
- CEPC
- Cinanserin
- Cyproheptadine
- Deramciclane
- Dotarizine
- Eltoprazine
- Esmirtazapine
- FR-260,010
- Ketanserin
- Ketotifen
- Latrepirdine
- Metitepine/Methiothepin
- Methysergide
- Pizotifen
- Ritanserin
- RS-102,221
- S-14,671
- SB-200,646
- SB-206,553
- SB-221,284
- SB-228,357
- SB-242,084
- SB-243,213
- SDZ SER-082
- Xylamidine
|
|
|
|
- 5-HT3
- 5-HT4
- 5-HT5
- 5-HT6
- 5-HT7 ligands
|
|
|
|
5-HT3
|
- Agonists: Piperazines: BZP
- Quipazine; Tryptamines: 2-Methyl-5-HT
- 5-CT; Others: Chlorophenylbiguanide
- Butanol
- Ethanol
- Halothane
- Isoflurane
- RS-56812
- SR-57,227
- SR-57,227-A
- Toluene
- Trichloroethane
- Trichloroethanol
- Trichloroethylene
- YM-31636
Antagonists: Antiemetics: AS-8112
- Alosetron
- Azasetron
- Batanopride
- Bemesetron
- Cilansetron
- Dazopride
- Dolasetron
- Granisetron
- Lerisetron
- Ondansetron
- Palonosetron
- Ramosetron
- Renzapride
- Tropisetron
- Zacopride
- Zatosetron; Atypical antipsychotics: Clozapine
- Olanzapine
- Quetiapine; Tetracyclic antidepressants: Amoxapine
- Mianserin
- Mirtazapine; Others: CSP-2503
- ICS-205,930
- MDL-72,222
- Memantine
- Nitrous Oxide
- Ricasetron
- Sevoflurane
- Tedatioxetine
- Thujone
- Tropanserin
- Vortioxetine
- Xenon
|
|
|
5-HT4
|
- Agonists: Gastroprokinetic Agents: Cinitapride
- Cisapride
- Dazopride
- Metoclopramide
- Mosapride
- Prucalopride
- Renzapride
- Tegaserod
- Velusetrag
- Zacopride; Others: 5-MT
- BIMU8
- CJ-033,466
- PRX-03140
- RS-67333
- RS-67506
- SL65.0155
- Antagonists: GR-113,808
- GR-125,487
- L-Lysine
- Piboserod
- RS-39604
- RS-67532
- SB-203,186
- SB-204,070
|
|
|
5-HT5A
|
- Agonists: Lysergamides: Ergotamine
- LSD; Tryptamines: 5-CT; Others: Valerenic Acid
Antagonists: Asenapine
- Latrepirdine
- Metitepine/Methiothepin
- Ritanserin
- SB-699,551
* Note that the 5-HT5B receptor is not functional in humans.
|
|
|
5-HT6
|
- Agonists: Lysergamides: Dihydroergotamine
- Ergotamine
- Lisuride
- LSD
- Mesulergine
- Metergoline
- Methysergide; Tryptamines: 2-Methyl-5-HT
- 5-BT
- 5-CT
- 5-MT
- Bufotenin
- E-6801
- E-6837
- EMD-386,088
- EMDT
- LY-586,713
- N-Methyl-5-HT
- Tryptamine; Others: WAY-181,187
- WAY-208,466
Antagonists: Antidepressants: Amitriptyline
- Amoxapine
- Clomipramine
- Doxepin
- Mianserin
- Nortriptyline; Atypical antipsychotics: Aripiprazole
- Asenapine
- Clorotepine
- Clozapine
- Fluperlapine
- Iloperidone
- Olanzapine
- Tiospirone; Typical antipsychotics: Chlorpromazine
- Loxapine; Others: BGC20-760
- BVT-5182
- BVT-74316
- Cerlapirdine
- EGIS-12,233
- GW-742,457
- Ketanserin
- Latrepirdine
- Lu AE58054
- Metitepine/Methiothepin
- MS-245
- PRX-07034
- Ritanserin
- Ro04-6790
- Ro 63-0563
- SB-258,585
- SB-271,046
- SB-357,134
- SB-399,885
- SB-742,457
|
|
|
5-HT7
|
- Agonists: Lysergamides: LSD; Tryptamines: 5-CT
- 5-MT
- Bufotenin; Others: 8-OH-DPAT
- AS-19
- Bifeprunox
- E-55888
- LP-12
- LP-44
- RU-24,969
- Sarizotan
Antagonists: Lysergamides: 2-Bromo-LSD
- Bromocriptine
- Dihydroergotamine
- Ergotamine
- Mesulergine
- Metergoline
- Methysergide; Antidepressants: Amitriptyline
- Amoxapine
- Clomipramine
- Imipramine
- Maprotiline
- Mianserin; Atypical antipsychotics: Amisulpride
- Aripiprazole
- Clorotepine
- Clozapine
- Olanzapine
- Risperidone
- Sertindole
- Tiospirone
- Ziprasidone
- Zotepine; Typical antipsychotics: Chlorpromazine
- Loxapine; Others: Butaclamol
- EGIS-12,233
- Ketanserin
- LY-215,840
- Metitepine/Methiothepin
- Pimozide
- Ritanserin
- SB-258,719
- SB-258,741
- SB-269,970
- SB-656,104
- SB-656,104-A
- SB-691,673
- SLV-313
- SLV-314
- Spiperone
- SSR-181,507
- Vortioxetine
|
|
|
|
|
Reuptake inhibitors
|
|
|
SERT
|
- Selective serotonin reuptake inhibitors (SSRIs): Alaproclate
- Citalopram
- Dapoxetine
- Desmethylcitalopram
- Desmethylsertraline
- Escitalopram
- Femoxetine
- Fluoxetine
- Fluvoxamine
- Indalpine
- Ifoxetine
- Litoxetine
- Lubazodone
- Omiloxetine
- Panuramine
- Paroxetine
- Pirandamine
- RTI-353
- Seproxetine
- Sertraline
- Vilazodone
- Vortioxetine
- Zimelidine; Serotonin-norepinephrine reuptake inhibitors (SNRIs): Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- Sibutramine
- Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors (SNDRIs): Brasofensine
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- NS-2359
- SEP-225289
- SEP-227,162
- Tedatioxetine
- Tesofensine; Tricyclic antidepressants (TCAs): Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- Nortriptyline
- Pipofezine
- Protriptyline
- Trimipramine; Tetracyclic antidepressants (TeCAs): Amoxapine; Piperazines: Nefazodone
- Trazodone; Antihistamines: Brompheniramine
- Chlorphenamine
- Diphenhydramine
- Mepyramine/Pyrilamine
- Pheniramine
- Tripelennamine; Opioids: Pethidine
- Methadone
- Propoxyphene; Others: Cocaine
- CP-39,332
- Cyclobenzaprine
- Dextromethorphan
- Dextrorphan
- EXP-561
- Fezolamine
- Mesembrine
- Nefopam
- PIM-35
- Pridefine
- Roxindole
- SB-649,915
- Tofenacin
- Ziprasidone
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VMAT
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- Ibogaine
- Reserpine
- Tetrabenazine
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Releasing agents
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- Aminoindanes: 5-IAI
- AMMI
- ETAI
- MDAI
- MDMAI
- MMAI
- TAI; Aminotetralins: 6-CAT
- 8-OH-DPAT
- MDAT
- MDMAT; Oxazolines: 4-Methylaminorex
- Aminorex
- Clominorex
- Fluminorex; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 2-Methyl-MDA
- 4-CAB
- 4-FA
- 4-FMA
- 4-HA
- 4-MTA
- 5-APDB
- 5-Methyl-MDA
- 6-APDB
- 6-Methyl-MDA
- AEMMA
- Amiflamine
- BDB
- BOH
- Brephedrone
- Butylone
- Chlorphentermine
- Cloforex
- Amfepramone
- Metamfepramone
- DCA
- DFMDA
- DMA
- DMMA
- EBDB
- EDMA
- Ethylone
- Etolorex
- Fenfluramine (Dexfenfluramine, Levofenfluramine)
- Flephedrone
- IAP
- IMP
- Iofetamine
- Lophophine
- MBDB
- MDA
- MDEA
- MDHMA
- MDMA
- MDMPEA
- MDOH
- MDPEA
- Mephedrone
- Methedrone
- Methylone
- MMA
- MMDA
- MMDMA
- MMMA
- NAP
- Norfenfluramine
- 4-TFMA
- pBA
- pCA
- pIA
- PMA
- PMEA
- PMMA
- TAP; Piperazines: 2C-B-BZP
- 2-BZP
- 3-MeOPP
- BZP
- DCPP
- MBZP
- mCPP
- MDBZP
- MeOPP
- Mepiprazole
- pCPP
- pFPP
- pTFMPP
- TFMPP; Tryptamines: 4-Methyl-αET
- 4-Methyl-αMT
- 5-CT
- 5-MeO-αET
- 5-MeO-αMT
- 5-MT
- αET
- αMT
- DMT
- Tryptamine (itself); Others: Indeloxazine
- Tramadol
- Viqualine
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Enzyme inhibitors
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Anabolism
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TPH
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AAAD
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- Benserazide
- Carbidopa
- Genistein
- Methyldopa
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Catabolism
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MAO
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- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A Selective: Amiflamine
- Bazinaprine
- Befloxatone
- Befol
- Brofaromine
- Cimoxatone
- Clorgiline
- Esuprone
- Harmala alkaloids (Harmine
- Harmaline
- Tetrahydroharmine
- Harman
- Norharman, etc)
- Methylene Blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima
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Others
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Precursors
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Cofactors
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- Ferrous iron (Fe2+)
- Magnesium (Mg2+)
- Tetrahydrobiopterin
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal phosphate)
- Vitamin B9 (Folic Acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
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Others
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- Activity enhancers: BPAP
- PPAP; Reuptake enhancers: Tianeptine
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