- 関
- adrenergic blocker、adrenergic receptor antagonist、adrenolytics、antiadrenergic agent、antiadrenergics
WordNet
- a drug that neutralizes or counteracts the effects of another drug
- a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
- drug that has the effects of epinephrine (同)adrenergic_drug
- relating to epinephrine (its release or action) (同)sympathomimetic
PrepTutorEJDIC
- 対立する人,敵対者,競争相手(opponent)
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/11/13 07:38:33」(JST)
[Wiki en表示]
An Adrenergic antagonist is a pharmaceutical substance that acts to inhibit the action of catecholamines at the adrenergic receptors. It is thus a type of sympatholytic. Many important and commonly prescribed medications are adrenergic antagonists, including prazosin and propanolol. Like all pharmacological receptor antagonists, adrenergic antagonists only show an effect when the receptor's effector is present.
It has the opposite effect as adrenergic agonists.
More specifically, they can be divided into:
- Alpha blockers
- Beta blockers
Structure Activity Relationship
If the amine on the Adrenergic agent has a substituent bigger than a tertiary butyl, then the compound becomes an adrenergic antagonist.[1]
References
- ^ Medicinal Chemistry of Adrenergics and Cholinergics
External links
- Adrenergic antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
|
Sympatholytic (and closely related) antihypertensives (C02)
|
|
Sympatholytics
(antagonize α-adrenergic
vasoconstriction) |
|
Central
|
|
α2 agonist
|
- Clonidine
- Guanabenz
- Guanfacine
- Methyldopa#
|
|
|
Adrenergic release inhibitors
|
- Bethanidine
- Bretylium
- Debrisoquine
- Guanadrel
- Guanazodine
- Guanethidine
- Guanoclor
- Guanazodine
- Guanoxabenz
- Guanoxan
|
|
|
Imidazoline receptor agonist
|
|
|
|
Ganglion-blocking/nicotinic antagonist
|
- Mecamylamine
- Pentolinium
- Trimethaphan
|
|
|
|
Peripheral
|
|
Indirect
|
|
MAOI
|
|
|
|
Adrenergic uptake inhibitor
|
- Bietaserpine
- Deserpidine
- Methoserpidine
- Rescinnamine
- Reserpine
|
|
|
Tyrosine hydroxylase inhibitor
|
|
|
|
|
Direct
|
|
α1 blockers
|
- Prazosin
- Indoramin
- Trimazosin
- Doxazosin
- Urapidil
|
|
|
Non-selective α blocker
|
|
|
|
|
|
| Other antagonists |
|
Serotonin antagonist
|
|
|
|
Endothelin antagonist (for PH)
|
- dual (Bosentan, Macitentan)
- selective (Ambrisentan, Sitaxentan)
|
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
anat (a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot
|
noco/syva/cong/lyvd/tumr, sysi/epon, injr
|
proc, drug (C2s+n/3/4/5/7/8/9)
|
|
|
|
|
Neuromodulation
|
|
| Types |
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Antagonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- Inverse agonist
- ♦ Transporter [Reuptake]: Enhancer (RE)
- Inhibitor (RI)
- Releaser (RA)
- ♦ Miscellaneous: Precursor
- Cofactor
|
|
| Classes |
|
Enzyme
|
see Enzyme inhibition
|
|
|
Ion channel
|
- Calcium channel blocker (CCB)
- Potassium channel blocker (PCB)
- Sodium channel blocker (SCB)
- Potassium channel opener (PCO)
|
|
|
Receptor &
transporter
|
|
BA/M
|
|
Adrenergic
|
- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2), β)
- Adrenergic reuptake inhibitor (ARI)
|
|
|
Dopaminergic
|
- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
|
|
|
Histaminergic
|
- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
|
|
|
Serotonergic
|
- Serotonin receptor agonist
- Serotonin Receptor Antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
|
|
|
|
AA
|
|
GABAergic
|
- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
|
|
|
Glutamatergic
|
- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
- Glutamate reuptake inhibitor
|
|
|
|
Cholinergic
|
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
|
|
|
Endocannabinoid
|
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
|
|
|
Opioidergic
|
- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
|
|
|
Other
|
- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
|
|
|
|
Miscellaneous
|
- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
|
|
|
|
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
- Hydroxyzine
- 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
- Fencamine
- Fencamfamine
- Hydroxybupropion
- 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
- Liafensine
- Methylnaphthidate
- Naphyrone
- NS-2359
- Perafensine
- 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
- Ethanol
- 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
- Brofaromine
- Cimoxatone
- Clorgiline
- Eprobemide
- 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
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- Activation of D2-like dopamine receptors inhibits GABA and glycinergic neurotransmission to pre-motor cardiac vagal neurons in the nucleus ambiguus.
- Dyavanapalli J, Byrne P, Mendelowitz D.SourceDepartment of Pharmacology & Physiology, The George Washington University, 2300 Eye Street NW, Washington, DC 20037, USA. Electronic address: Jhansi82@gwu.edu.
- Neuroscience.Neuroscience.2013 Sep 5;247:213-26. doi: 10.1016/j.neuroscience.2013.05.039. Epub 2013 May 29.
- The parasympathetic control of heart rate arises from premotor cardiac vagal neurons (CVNs) located in the nucleus ambiguus (NA). Previous microinjection studies in NA show that dopamine evokes a decrease in heart rate, but the underlying mechanisms responsible for these responses were not identifie
- PMID 23727508
- Participation of citral in the bronchodilatory effect of ginger oil and possible mechanism of action.
- Mangprayool T, Kupittayanant S, Chudapongse N.SourceInstitute of Science, Suranaree University of Technology, Nakhon Ratchasima 30000, Thailand; The Center for Scientific and Technological Equipment, Suranaree University of Technology, Nakhon Ratchasima 30000, Thailand.
- Fitoterapia.Fitoterapia.2013 Sep;89:68-73. doi: 10.1016/j.fitote.2013.05.012. Epub 2013 May 17.
- The extract of ginger, the rhizomes of Zingiber officinale Roscoe (Zingiberaceae), has been reported to possess anti-hyperactivity and anti-inflammation on airway. The present study described brochodilatory activity of ginger oil and identified its active compound. Ginger oil was extracted by hydro-
- PMID 23685048
- Corticotropin-releasing factor (CRF) and α 2 adrenergic receptors mediate heroin withdrawal-potentiated startle in rats.
- Park PE, Vendruscolo LF, Schlosburg JE, Edwards S, Schulteis G, Koob GF.SourceCommittee on the Neurobiology of Addictive Disorders, The Scripps Research Institute, La Jolla, CA, USA.
- The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2013 Sep;16(8):1867-75. doi: 10.1017/S1461145713000308. Epub 2013 Apr 16.
- Anxiety is one of the early symptoms of opioid withdrawal and contributes to continued drug use and relapse. The acoustic startle response (ASR) is a component of anxiety that has been shown to increase during opioid withdrawal in both humans and animals. We investigated the role of corticotropin-re
- PMID 23590881
Japanese Journal
- 交感神経α1遮断薬,交感神経刺激薬,副交感神経作動薬 (特集 わかりやすい緑内障薬物のお話)
- 薬物治療--RAS系抑制薬とβ遮断薬 (特集 心不全診療--予防と治療の最前線)
Related Links
- An Adrenergic antagonist is a pharmaceutical substance that acts to inhibit the action of the adrenergic receptors. It is thus a type of sympatholytic. It has the opposite effect as adrenergic agonists. ...
Related Pictures
★リンクテーブル★
[★]
- 関
- adrenergic antagonist、adrenergic receptor antagonist、adrenolytics、antiadrenergic agent、antiadrenergics
[★]
- 英
- adrenergic antagonist、adrenergic blocker
- 関
- アドレナリン拮抗薬、アドレナリン受容体拮抗薬、抗アドレナリン薬、アドレナリン受容体遮断薬
[★]
- 関
- adrenergic antagonist、adrenergic blocker、adrenolytics、antiadrenergic agent、antiadrenergics
[★]
抗アドレナリン薬
- 関
- adrenergic antagonist、adrenergic blocker、adrenergic receptor antagonist、adrenolytic、antiadrenergic agent、antiadrenergics
[★]
抗アドレナリン薬
- 関
- adrenergic antagonist、adrenergic blocker、adrenergic receptor antagonist、adrenolytic、adrenolytics、antiadrenergic agent
[★]
- 関
- beta-adrenergic blocker、beta-adrenergic blocking agent、beta-adrenergic receptor antagonist、beta-antagonist、beta-blocker
[★]
- 関
- alpha-adrenergic blocking agent、alpha-adrenergic receptor antagonist、alpha-blocker
[★]
アドレナリン受容体刺激薬、アドレナリン作用薬
- 関
- adrenergic、adrenergic agent、adrenergic agonist、adrenergic drug、adrenergic receptor agonist
[★]