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- diethylpropion
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2012/06/18 13:44:33」(JST)
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Amfepramone
|
Systematic (IUPAC) name |
(RS)-2-diethylamino-1-phenylpropan-1-one |
Clinical data |
Trade names |
Tenuate |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a682037 |
Pregnancy cat. |
B |
Legal status |
Schedule IV (US) |
Routes |
Oral |
Identifiers |
CAS number |
134-80-5 Y |
ATC code |
A08AA03 |
PubChem |
CID 7029 |
DrugBank |
DB00937 |
ChemSpider |
6762 Y |
UNII |
19V2PL39NG Y |
KEGG |
D07444 N |
ChEBI |
CHEBI:4530 Y |
ChEMBL |
CHEMBL1194666 N |
Synonyms |
Diethylpropion |
Chemical data |
Formula |
C13H19NO |
Mol. mass |
205.30 g/mol |
|
InChI
-
InChI=1S/C13H19NO/c1-4-14(5-2)11(3)13(15)12-9-7-6-8-10-12/h6-11H,4-5H2,1-3H3 Y
Key:XXEPPPIWZFICOJ-UHFFFAOYSA-N Y
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N (what is this?) (verify)
|
Amfepramone (INN, other names diethylcathinone and diethylpropion, trade names Anorex, Linea, Nobesine, Prefamone, Regenon, Tepanil, Tenuate), is a stimulant drug of the phenethylamine, amphetamine, and cathinone chemical classes that is used as an appetite suppressant.
Contents
- 1 Pharmacology
- 2 Abuse
- 3 Legality
- 4 Chemistry
- 5 See also
- 6 References
|
Pharmacology
Amfepramone itself lacks any affinity for the monoamine transporters and instead functions as a prodrug to ethcathinone.[1] Ethcathinone (and therefore amfepramone as well) is a very weak dopaminergic and serotonergic, and is approximately 10x and 20x stronger on norepinephrine in comparison, respectively.[1] As a result, ethcathinone and amfepramone can essentially be considered selective norepinephrine releasing agents (NRAs).
Abuse
Amfepramone is believed to have relatively low abuse potential.[2][3][4][5]
Legality
Amfepramone is classified as a Schedule IV controlled substance in the United States. In the UK Amfepramone is a class C drug.[6]
Chemistry
- Propiophenone is brominated to produce α-bromopropiophenone.
- This is reacted with diethylamine to yield the product, diethylpropion.[7][8]
See also
References
- ^ a b Rothman, R. B.; Baumann, M. H. (2006). "Therapeutic Potential of Monoamine Transporter Substrates". Current Topics in Medicinal Chemistry 6 (17): 1845–1859. DOI:10.2174/156802606778249766. PMID 17017961. http://www.bentham-direct.org/pages/content.php?CTMC/2006/00000006/00000017/0004R.SGM.
- ^ Cohen, S. (1977). "Diethylpropion (Tenuate): An Infrequently Abused Anorectic". Psychosomatics 18 (1): 28–33. PMID 850721. http://psy.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=850721.
- ^ Jasinski, D. R.; Krishnan, S. (June 2009). "Abuse Liability and Safety of Oral Lisdexamfetamine Dimesylate in Individuals with a History of Stimulant Abuse". Journal of Psychopharmacology 23 (4): 419–427. DOI:10.1177/0269881109103113. PMID 19329547.
- ^ "Tepanil (diethylpropion hydrochloride) tablet, extended release". Dailymed. National Institutes of Health. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=1611.
- ^ Caplan, J. (May 1963). "Habituation to Diethylpropion (Tenuate)". Canadian Medical Association Journal 88: 943–944. PMC 1921278. PMID 14018413. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1921278.
- ^ "Class C Drugs". Schedule 2 Controlled Drugs. UK Legislation. http://www.legislation.gov.uk/ukpga/1971/38/schedule/2.
- ^ US patent 3001910, "Anorexigenic Propiophenones", issued 1961-09-26, assigned to Temmler-Werke
- ^ Hyde, J. F.; Browning, E.; Adams, R. (1928). "Synthetic Homologs of d,l-Ephedrine". Journal of the American Chemical Society 50 (8): 2287–2292. DOI:10.1021/ja01395a032. edit
Stimulants (N06B)
|
|
Adamantanes |
- Adaphenoxate
- Adapromine
- Amantadine
- Bromantane
- Chlodantane
- Gludantane
- Memantine
- Midantane
|
|
Adenosine antagonists |
- 8-Chlorotheophylline
- 8-Cyclopentyltheophylline
- 8-Phenyltheophylline
- Aminophylline
- Caffeine
- CGS-15943
- Dimethazan
- Paraxanthine
- SCH-58261
- Theobromine
- Theophylline
|
|
Alkylamines |
- Cyclopentamine
- Cypenamine
- Cyprodenate
- Heptaminol
- Isometheptene
- Methylhexaneamine
- Octodrine
- Propylhexedrine
- Tuaminoheptane
|
|
Arylcyclohexylamines |
- Benocyclidine
- Dieticyclidine
- Esketamine
- Eticyclidine
- Gacyclidine
- Ketamine
- Phencyclamine
- Phencyclidine
- Rolicyclidine
- Tenocyclidine
- Tiletamine
|
|
Benzazepines |
- 6-Br-APB
- SKF-77434
- SKF-81297
- SKF-82958
|
|
Cholinergics |
- A-84,543
- A-366,833
- ABT-202
- ABT-418
- AR-R17779
- Altinicline
- Anabasine
- Arecoline
- Cotinine
- Cytisine
- Dianicline
- Epibatidine
- Epiboxidine
- GTS-21
- Ispronicline
- Nicotine
- PHA-543,613
- PNU-120,596
- PNU-282,987
- Pozanicline
- Rivanicline
- Sazetidine A
- SIB-1553A
- SSR-180,711
- TC-1698
- TC-1827
- TC-2216
- TC-5619
- Tebanicline
- UB-165
- Varenicline
- WAY-317,538
|
|
Convulsants |
- Anatoxin-a
- Bicuculline
- DMCM
- Flurothyl
- Gabazine
- Pentetrazol
- Picrotoxin
- Strychnine
- Thujone
|
|
Eugeroics |
- Adrafinil
- Armodafinil
- CRL-40941
- Modafinil
|
|
Oxazolines |
- 4-Methylaminorex
- Aminorex
- Clominorex
- Cyclazodone
- Fenozolone
- Fluminorex
- Pemoline
- Thozalinone
|
|
Phenethylamines |
|
|
Piperazines |
- 2C-B-BZP
- BZP
- CM156
- DBL-583
- GBR-12783
- GBR-12935
- GBR-13069
- GBR-13098
- GBR-13119
- MeOPP
- MBZP
- Vanoxerine
|
|
Piperidines |
- 1-Benzyl-4-(2-(diphenylmethoxy)ethyl)piperidine
- 1-(3,4-Dichlorophenyl)-1-(piperidin-2-yl)butane
- 2-Benzylpiperidine
- 2-Methyl-3-phenylpiperidine
- 3,4-Dichloromethylphenidate
- 4-Benzylpiperidine
- 4-Methylmethylphenidate
- Desoxypipradrol
- Difemetorex
- Diphenylpyraline
- Ethylphenidate
- Methylnaphthidate
- Methylphenidate (Dexmethylphenidate)
- N-Methyl-3ß-propyl-4ß-(4-chlorophenyl)piperidine
- Nocaine
- Phacetoperane
- Pipradrol
- SCH-5472
|
|
Pyrrolidines |
- 2-Diphenylmethylpyrrolidine
- a-PPP
- a-PBP
- a-PVP
- Diphenylprolinol
- MDPPP
- MDPBP
- MDPV
- MPBP
- MPHP
- MPPP
- MOPPP
- Naphyrone
- PEP
- Prolintane
- Pyrovalerone
|
|
Tropanes |
- 3-CPMT
- 3'-Chloro-3a-(diphenylmethoxy)tropane
- 3-Pseudotropyl-4-fluorobenzoate
- 4'-Fluorococaine
- AHN-1055
- Altropane (IACFT)
- Brasofensine
- CFT (WIN 35,428)
- ß-CIT (RTI-55)
- Cocaethylene
- Cocaine
- Dichloropane (RTI-111)
- Difluoropine
- FE-ß-CPPIT
- FP-ß-CPPIT
- Ioflupane (123I)
- Norcocaine
- PIT
- PTT
- RTI-31
- RTI-32
- RTI-51
- RTI-105
- RTI-112
- RTI-113
- RTI-117
- RTI-120
- RTI-121 (IPCIT)
- RTI-126
- RTI-150
- RTI-154
- RTI-171
- RTI-177
- RTI-183
- RTI-193
- RTI-194
- RTI-199
- RTI-202
- RTI-204
- RTI-229
- RTI-241
- RTI-336
- RTI-354
- RTI-371
- RTI-386
- Salicylmethylecgonine
- Tesofensine
- Troparil (ß-CPT, WIN 35,065-2)
- Tropoxane
- WF-23
- WF-33
- WF-60
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Others |
- 1-(Thiophen-2-yl)-2-aminopropane
- 2-Amino-1,2-dihydronaphthalene
- 2-Aminoindane
- 2-Aminotetralin
- 2-MDP
- 2-Phenylcyclohexylamine
- 2-Phenyl-3,6-dimethylmorpholine
- 3-Benzhydrylmorpholine
- 3,3-Diphenylcyclobutanamine
- 5-(2-Aminopropyl)indole
- 5-Iodo-2-aminoindane
- AL-1095
- Amfonelic acid
- Amineptine
- Amiphenazole
- Atipamezole
- Atomoxetine
- Bemegride
- Benzydamine
- BTQ
- BTS 74,398
- Camfetamine
- Carphedon
- Ciclazindol
- Cilobamine
- Clofenciclan
- Cropropamide
- Crotetamide
- Cypenamine
- D-161
- Diclofensine
- Dimethocaine
- Efaroxan
- Etamivan
- EXP-561
- Fencamfamine
- Fenpentadiol
- Feprosidnine
- G-130
- Gamfexine
- Gilutensin
- GSK1360707F
- GYKI-52895
- Hexacyclonate
- Idazoxan
- Indanorex
- Indatraline
- JNJ-7925476
- JZ-IV-10
- Lazabemide
- Leptacline
- Levopropylhexedrine
- Lomevactone
- LR-5182
- Mazindol
- Meclofenoxate
- Medifoxamine
- Mefexamide
- Mesocarb
- Methastyridone
- Methiopropamine
- N-Methyl-3-phenylnorbornan-2-amine
- Nefopam
- Nikethamide
- Nomifensine
- O-2172
- Oxaprotiline
- Phthalimidopropiophenone
- PNU-99,194
- Propylhexedrine
- PRC200-SS
- Rasagiline
- Rauwolscine
- Rubidium chloride
- Setazindol
- Tametraline
- Tandamine
- Trazium
- UH-232
- Yohimbine
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See also Sympathomimetic amines
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|
Antiobesity agents/Anorectics (A08)
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|
Central |
Stimulants
|
- 4-Methylamphetamine
- Amfecloral
- Amfepentorex
- Amfepramone
- Aminorex
- Amphetamine
- Amphetaminil
- Atomoxetine
- Benfluorex‡
- Benzphetamine
- Bupropion
- Cathine
- Cathinone
- Chlorphentermine
- Ciclazindol
- Clobenzorex
- Cloforex
- Clominorex
- Clortermine
- Dexfenfluramine
- Dextroamphetamine
- Dextromethamphetamine
- Dexmethylphenidate
- Difemetorex
- Dimethylcathinone
- Diphemethoxidine
- Ephedrine
- Ephedra
- Ethylamphetamine
- Etolorex
- Fenbutrazate
- Fencamfamine
- Fenethylline
- Fenfluramine (+phentermine)
- Fenproporex
- Fludorex
- Fluminorex
- Furfenorex
- Indanorex
- Khat
- Levopropylhexedrine
- Lisdexamfetamine
- Manifaxine
- Mazindol
- Mefenorex
- Methamphetamine
- Methylphenidate
- Norfenfluramine
- Pemoline
- Pentorex (Phenpentermine)
- Phendimetrazine
- Phenethylamine
- Phenmetrazine
- Phentermine
- Phenylpropanolamine
- Pipradrol
- Prolintane
- Propylhexedrine
- Pseudoephedrine
- Pyrovalerone
- Radafaxine
- Reboxetine
- Setazindol
- Sibutramine
- Synephrine
- Tesofensine
- Viloxazine
- Xylopropamine
- Zylofuramine
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Cannabinoids
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Drinabant • Ibipinabant • Otenabant • Rimonabant • Rosonabant • Surinabant • Taranabant
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Others
|
5-HTP • Galactomannan (Guar gum) • Glucomannan • L-DOPA • L-Phenylalanine • L-Tryptophan • L-Tyrosine • Lorcaserin • Lu AA-33810 • Metformin • Naltrexone • Naloxone • Oxyntomodulin • P57 • Peptide YY • Topiramate • Yohimbine (Yohimbe) • Zonisamide
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Peripheral |
Cetilistat • Dinitrophenol‡ • Dirlotapide • Mitratapide • Oleoyl-estrone • Orlistat • Simmondsin • Sterculia
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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noco, nuvi, sysi/epon, met
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Neurotoxins
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Animal toxins |
- Batrachotoxin
- Bestoxin
- Birtoxin
- Bungarotoxin
- Charybdotoxin
- Conotoxin
- Saxitoxin
- Tetrodotoxin
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Bacterial toxins |
- Botulinum toxin
- Tetanospasmin
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Bacterial toxins |
- Fungal toxins
- Bicuculline
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Plant toxins |
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Pesticides |
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Nerve agents |
- Cyclosarin
- EA-3148
- Novichok agent
- Sarin
- Soman
- Tabun (nerve agent)
- VE (nerve agent)
- VG (nerve agent)
- VM (nerve agent)
- VR (nerve agent)
- VX (nerve agent)
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Neurotransmitters
and precursors |
- Dopamine
- Glutamate
- L-Tyrosine
- L-Phenylalanine
- L-DOPA (Levodopa)
- L-Glutamine
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Neurotoxic drugs |
- 1,4-BD
- 5,7-DHT
- 6-OHDA
- αET
- αMT
- Amphetamine
- Dizocilpine (MK-801)
- DSP-4
- Ethanol
- GBL
- GHB
- Ibotenic Acid
- Ketamine
- Lisdexamfetamine
- Methamphetamine
- MBDB
- MDA
- MDEA
- MDMA (Ecstasy)
- MPP+
- MPTP
- Norsalsolinol
- PBA
- PCA
- PIA
- Phencyclidine (PCP)
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Adrenergics
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Receptor ligands
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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.
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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
- 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.
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β
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Reuptake inhibitors
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NET
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- 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
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VMAT
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- Ibogaine
- Reserpine
- Tetrabenazine
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Enzyme inhibitors
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Anabolism
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PAH
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TH
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- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD
|
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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DBH
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- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
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PNMT
|
- CGS-19281A
- SKF-64139
- SKF-7698
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Catabolism
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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.
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COMT
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- Entacapone
- Nitecapone
- Tolcapone
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Others
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Precursors
|
- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
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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+)
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Others
|
- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
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List of adrenergic drugs
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Dopaminergics
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Receptor ligands
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Agonists
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- Adamantanes: Amantadine
- Memantine
- Rimantadine; Aminotetralins: 7-OH-DPAT
- 8-OH-PBZI
- Rotigotine
- UH-232; Benzazepines: 6-Br-APB
- Fenoldopam
- SKF-38,393
- SKF-77,434
- SKF-81,297
- SKF-82,958
- SKF-83,959; Ergolines: Bromocriptine
- Cabergoline
- Dihydroergocryptine
- Epicriptine
- Lisuride
- LSD
- Pergolide; Dihydrexidine derivatives: 2-OH-NPA
- A-86,929
- Ciladopa
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine; Others: A-68,930
- A-77636
- A-412,997
- ABT-670
- ABT-724
- Aplindore
- Apomorphine
- Aripiprazole
- Bifeprunox
- BP-897
- CY-208,243
- Dizocilpine
- Etilevodopa
- Flibanserin
- Ketamine
- Melevodopa
- Modafinil
- Pardoprunox
- Phencyclidine
- PD-128,907
- PD-168,077
- PF-219,061
- Piribedil
- Pramipexole
- Propylnorapomorphine
- Pukateine
- Quinagolide
- Quinelorane
- Quinpirole
- RDS-127
- Ro10-5824
- Ropinirole
- Rotigotine
- Roxindole
- Salvinorin A
- SKF-89,145
- Sumanirole
- Terguride
- Umespirone
- WAY-100,635
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Antagonists
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- Typical antipsychotics: Acepromazine
- Azaperone
- Benperidol
- Bromperidol
- Clopenthixol
- Chlorpromazine
- Chlorprothixene
- Droperidol
- Flupentixol
- Fluphenazine
- Fluspirilene
- Haloperidol
- Loxapine
- Mesoridazine
- Methotrimeprazine
- Nemonapride
- Penfluridol
- Perazine
- Periciazine
- Perphenazine
- Pimozide
- Prochlorperazine
- Promazine
- Sulforidazine
- Sulpiride
- Sultopride
- Thioridazine
- Thiothixene
- Trifluoperazine
- Triflupromazine
- Trifluperidol
- Zuclopenthixol; Atypical antipsychotics: Amisulpride
- Asenapine
- Blonanserin
- Cariprazine
- Carpipramine
- Clocapramine
- Clorotepine
- Clozapine
- Gevotroline
- Iloperidone
- Lurasidone
- Melperone
- Molindone
- Mosapramine
- Olanzapine
- Paliperidone
- Perospirone
- Piquindone
- Quetiapine
- Remoxipride
- Risperidone
- Sertindole
- Tiospirone
- Ziprasidone
- Zotepine; Antiemetics: AS-8112
- Alizapride
- Bromopride
- Clebopride
- Domperidone
- Metoclopramide
- Thiethylperazine; Others: Amoxapine
- Buspirone
- Butaclamol
- Ecopipam
- EEDQ
- Eticlopride
- Fananserin
- L-745,870
- Nafadotride
- Nuciferine
- PNU-99,194
- Raclopride
- Sarizotan
- SB-277,011-A
- SCH-23,390
- SKF-83,959
- Sonepiprazole
- Spiperone
- Spiroxatrine
- Stepholidine
- Tetrahydropalmatine
- Tiapride
- UH-232
- Yohimbine
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Reuptake inhibitors
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Plasmalemmal
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DAT inhibitors
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- Piperazines: DBL-583
- GBR-12,935
- Nefazodone
- Vanoxerine; Piperidines: BTCP
- Desoxypipradrol
- Dextromethylphenidate
- Difemetorex
- Ethylphenidate
- Methylnaphthidate
- Methylphenidate
- Phencyclidine
- Pipradrol; Pyrrolidines: Diphenylprolinol
- MDPV
- Naphyrone
- Prolintane
- Pyrovalerone; Tropanes: Altropane
- Brasofensine
- CFT
- Cocaine
- Dichloropane
- Difluoropine
- FE-β-CPPIT
- FP-β-CPPIT
- Ioflupane (123I)
- Iometopane
- RTI-112
- RTI-113
- RTI-121
- RTI-126
- RTI-150
- RTI-177
- RTI-229
- RTI-336
- Tenocyclidine
- Tesofensine
- Troparil
- Tropoxane
- WF-11
- WF-23
- WF-31
- WF-33; Others: Adrafinil
- Armodafinil
- Amfonelic acid
- Amineptine
- Benzatropine
- Bromantane
- BTQ
- BTS-74,398
- Bupropion
- Ciclazindol
- Diclofensine
- Dimethocaine
- Diphenylpyraline
- Dizocilpine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- Etybenzatropine
- EXP-561
- Fencamine
- Fencamfamine
- Fezolamine
- GYKI-52,895
- Indatraline
- Ketamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Mazindol
- Medifoxamine
- Mesocarb
- Modafinil
- Nefopam
- Nomifensine
- NS-2359
- O-2172
- Pridefrine
- Propylamphetamine
- Radafaxine
- SEP-225,289
- SEP-227,162
- Sertraline
- Sibutramine
- Tametraline
- Tedatioxetine
- Tripelennamine
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Vesicular
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VMAT inhibitors
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- Deserpidine
- Ibogaine
- Reserpine
- Tetrabenazine
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|
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Allosteric modulators
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|
- Quinazolinamines: SoRI-9804
- SoRI-20040
- SoRI-20041
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Enzyme inhibitors
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Anabolism
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PAH inhibitors
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|
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TH inhibitors
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- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD/DDC inhibitors
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- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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|
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Catabolism
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MAO inhibitors
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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
- Methylene Blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective: D-Deprenyl
- L-Deprenyl (Selegiline)
- Ladostigil
- Lazabemide
- Milacemide
- Pargyline
- Rasagiline
- Safinamide
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COMT inhibitors
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- Entacapone
- Nitecapone
- Tolcapone
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DBH inhibitors
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- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Tropolone
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Others
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Precursors
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- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa)
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Cofactors
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- Ferrous iron (Fe2+)
- 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; Toxins: 6-OHDA
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|
|
List of dopaminergic drugs
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|
UpToDate Contents
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English Journal
- Vulnerability to dietary n-3 polyunsaturated fatty acid deficiency after exposure to early stress in rats.
- Ferreira CF, Bernardi JR, Krolow R, Arcego DM, Fries GR, de Aguiar BW, Senter G, Kapczinski FP, Silveira PP, Dalmaz C.SourcePrograma de Pós-Graduação em Ciências Biológicas: Neurociências, Instituto de Ciências Básicas da Saúde (ICBS), Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, RS, Brazil; Laboratório de Neurobiologia do Estresse, Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, RS, Brazil; Núcleo de Estudos da Saúde da Criança e do Adolescente, Hospital de Clínicas de Porto Alegre (HCPA), Faculdade de Medicina, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil. Electronic address: neurocientista@hotmail.com.
- Pharmacology, biochemistry, and behavior.Pharmacol Biochem Behav.2013 Jun;107C:11-19. doi: 10.1016/j.pbb.2013.03.006. Epub 2013 Mar 26.
- The exposure to adverse events early in life may affect brain development. Omega-3 polyunsaturated fatty acid (n-3 PUFA) deficiency has been linked to the development of mood and anxiety disorders. The aim of this study was to examine the interaction between variations in the early environment (hand
- PMID 23537731
- Lorcaserin: a novel serotonin 2C agonist for the treatment of obesity.
- Nigro SC, Luon D, Baker WL.SourceUniversity of Connecticut, Schools of Pharmacy and Medicine , Storrs and Farmington, CT , USA.
- Current medical research and opinion.Curr Med Res Opin.2013 May 10. [Epub ahead of print]
- Abstract Background: Obesity has become an epidemic in the United States and its prevalence continues to increase. Adjunctive treatment with pharmacotherapy is often reserved for individuals who fail to achieve their intended weight goals with diet and exercise alone. Current approved therapies for
- PMID 23574263
- The use of appetite suppressants among health sciences undergraduate students in Southern Brazil.
- Zubaran C, Lazzaretti R.SourceThe Biological and Health Sciences Center, Universidade de Caxias do Sul, Caxias do Sul, RS, Brasil.
- Einstein (Sao Paulo, Brazil).Einstein (Sao Paulo).2013 Mar;11(1):47-52.
- OBJECTIVE: To investigate the prevalence of appetite suppressant use among health sciences students in Southern Brazil.METHODS: Undergraduate students (n=300) from seven health science undergraduate courses of the Universidade de Caxias do Sul completed a questionnaire about the use of substances to
- PMID 23579743
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