Dopamine antagonist

Dopamine antagonist: Skeletal formula of clozapine, the first atypical antipsychotic, a dopamine antagonist.

A dopamine antagonist is a drug which blocks dopamine receptors by receptor antagonism. There are five known types of dopamine receptors in the human body; they are found in the brain, peripheral nervous system, blood vessels, gastrointestinal tract^[1] and the kidney.

Contents

1 Uses and examples

2 Side effects

3 Examples

4 References

5 External links

Uses and examples

Used as atypical antipsychotics (coupled with serotonin antagonist effects): clozapine, risperidone, olanzapine, quetiapine, and ziprasidone

Used as antiemetics: metoclopramide, droperidol, domperidone

Used as tricyclic antidepressants: amoxapine, clomipramine

Side effects

Parkinsonism – due to effects on the nigrostriatal pathway

Hyperprolactinaemia – due to effects on the tuberoinfundibular pathway

Tardive dyskinesia (long term use)

galactorrhea - due to removal of dopamine-mediated inhibition of prolactin release from lactotroph cells in the anterior pituitary

Other side effects may include menstrual dysfunction, low libido, and impotence.

Examples

Examples of Dopamine antagonists include:^[2]

acepromazine

amisulpride

amoxapine

azaperone

benperidol

bromopride

butaclamol

clomipramine (mild)

chlorpromazine

chlorprothixene

clopenthixol

domperidone

droperidol

eticlopride

flupenthixol

fluphenazine

fluspirilene

haloperidol

iodobenzamide

loxapine

mesoridazine

levomepromazine

metoclopramide

nafadotride

nemonapride

penfluridol

perazine

perphenazine

pimozide

prochlorperazine

promazine

raclopride

remoxipride

risperidone

spiperone

spiroxatrine

stepholidine

sulpiride

sultopride

tetrahydropalmatine

thiethylperazine

thioridazine

thiothixene

tiapride

trifluoperazine

trifluperidol

triflupromazine

ziprasidone

References

^ http://www.experts.umich.edu/grantDetail.asp?t=ep1&id=2680068&o_id=&n=Bitar%2C+Khalil+N&u_id=1335

^ MeSH list of agents 82018492

External links

MeSH Dopamine+antagonists

v · d · eDopaminergics

Receptor ligands

Agonists

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 • Lisuride • LSD • Pergolide; Dihydrexidine derivatives: 2-OH-NPA • A-86,929 • Ciladopa • Dihydrexidine • Dinapsoline • Dinoxyline • Doxanthrine; Others: A-68,930 • A-77,636 • 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

Antagonists

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 • 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

Reuptake inhibitors

Plasmalemmal

DAT inhibitors

Piperazines: DBL-583 • GBR-12,935 • Nefazodone • Vanoxerine; Piperidines: BTCP • Desoxypipradrol • Dextromethylphenidate • Difemetorex • Ethylphenidate • Methylnaphthidate • Methylphenidate • Phencyclidine • Pipradrol; Pyrrolidines: Diphenylprolinol • Methylenedioxypyrovalerone (MDPV) • Naphyrone • Prolintane • Pyrovalerone; Tropanes: β-CPPIT • 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 (Benztropine) • Bromantane • BTQ • BTS-74,398 • Bupropion (Amfebutamone) • Ciclazindol • Diclofensine • Dimethocaine • Diphenylpyraline • Dizocilpine • DOV-102,677 • DOV-21,947 • DOV-216,303 • Etybenzatropine (Ethylbenztropine) • 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 • Tripelennamine

Vesicular

VMAT inhibitors

Deserpidine • Ibogaine • Reserpine • Tetrabenazine

Releasing agents

Morpholines: Fenbutrazate • Morazone • Phendimetrazine • Phenmetrazine; Oxazolines: 4-Methylaminorex (4-MAR, 4-MAX) • Aminorex • Clominorex • Cyclazodone • Fenozolone • Fluminorex • Pemoline • Thozalinone; Phenethylamines (also amphetamines, cathinones, phentermines, etc): 2-Hydroxyphenethylamine (2-OH-PEA) • 4-CAB • 4-Methylamphetamine (4-MA) • 4-Methylmethamphetamine (4-MMA) • Alfetamine • Amfecloral • Amfepentorex • Amfepramone • Amphetamine (Dextroamphetamine, Levoamphetamine) • Amphetaminil • β-Methylphenethylamine (β-Me-PEA) • Benzodioxolylbutanamine (BDB) • Benzodioxolylhydroxybutanamine (BOH) • Benzphetamine • Buphedrone • Butylone • Cathine • Cathinone • Clobenzorex • Clortermine • D-Deprenyl • Dimethoxyamphetamine (DMA) • Dimethoxymethamphetamine (DMMA) • Dimethylamphetamine • Dimethylcathinone (Dimethylpropion, metamfepramone) • Ethcathinone (Ethylpropion) • Ethylamphetamine • Ethylbenzodioxolylbutanamine (EBDB) • Ethylone • Famprofazone • Fenethylline • Fenproporex • Flephedrone • Fludorex • Furfenorex • Hordenine • Lophophine (Homomyristicylamine) • Mefenorex • Mephedrone • Methamphetamine (Desoxyephedrine, Methedrine; Dextromethamphetamine, Levomethamphetamine) • Methcathinone (Methylpropion) • Methedrone • Methoxymethylenedioxyamphetamine (MMDA) • Methoxymethylenedioxymethamphetamine (MMDMA) • Methylbenzodioxolylbutanamine (MBDB) • Methylenedioxyamphetamine (MDA, tenamfetamine) • Methylenedioxyethylamphetamine (MDEA) • Methylenedioxyhydroxyamphetamine (MDOH) • Methylenedioxymethamphetamine (MDMA) • Methylenedioxymethylphenethylamine (MDMPEA, homarylamine) • Methylenedioxyphenethylamine (MDPEA, homopiperonylamine) • Methylone • Ortetamine • Parabromoamphetamine (PBA) • Parachloroamphetamine (PCA) • Parafluoroamphetamine (PFA) • Parafluoromethamphetamine (PFMA) • Parahydroxyamphetamine (PHA) • Paraiodoamphetamine (PIA) • Paredrine (Norpholedrine, Oxamphetamine) • Phenethylamine (PEA) • Pholedrine • Phenpromethamine • Prenylamine • Propylamphetamine • Tiflorex (Flutiorex) • Tyramine (TRA) • Xylopropamine • Zylofuramine; Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP) • Benzylpiperazine (BZP) • Methoxyphenylpiperazine (MeOPP, paraperazine) • Methylbenzylpiperazine (MBZP) • Methylenedioxybenzylpiperazine (MDBZP, piperonylpiperazine); Others: 2-Amino-1,2-dihydronaphthalene (2-ADN) • 2-Aminoindane (2-AI) • 2-Aminotetralin (2-AT) • 4-Benzylpiperidine (4-BP) • 5-IAI • Clofenciclan • Cyclopentamine • Cypenamine • Cyprodenate • Feprosidnine • Gilutensin • Heptaminol • Hexacyclonate • Indanylaminopropane (IAP) • Indanorex • Isometheptene • Methylhexanamine • Naphthylaminopropane (NAP) • Octodrine • Phthalimidopropiophenone • Propylhexedrine (Levopropylhexedrine) • Tuaminoheptane (Tuamine)

Enzyme inhibitors

Anabolism

PAH inhibitors

3,4-Dihydroxystyrene

TH inhibitors

3-Iodotyrosine • Aquayamycin • Bulbocapnine • Metirosine • Oudenone

AAAD/DDC inhibitors

Benserazide • Carbidopa • Genistein • Methyldopa

Catabolism

MAO inhibitors

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

COMT inhibitors

Entacapone • Tolcapone

DBH inhibitors

Disulfiram • Dopastin • Fusaric acid • Nepicastat • Tropolone

Others

Precursors

L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa)

Cofactors

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⁺)

Others

Activity enhancers: Benzofuranylpropylaminopentane (BPAP) • Phenylpropylaminopentane (PPAP); Toxins: Oxidopamine (6-Hydroxydopamine)

List of dopaminergic drugs

v · d · eNeuromodulation

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) • Serotonin reuptake enhancer (SRE)

AA

GABAergic

GABA receptor agonist • GABA receptor antagonist • GABA reuptake inhibitor (GRI)

Glutamatergic

Glutamate receptor agonist (AMPA) • Glutamate receptor antagonist (NMDA)

Cholinergic

Acetylcholine receptor agonist (Muscarinic, Nicotinic) • Acetylcholine receptor antagonist (Muscarinic, Nicotinic (Ganglionic, Muscular))

Endocannabinoid

Cannabinoid receptor agonist • Cannabinoid receptor antagonist

Opioid

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)

v · d · eDrugs for functional gastrointestinal disorders (A03)

Drugs for
functional bowel disorders

Antimuscarinics

Tertiary
amino group

Oxyphencyclimine • Camylofin • Mebeverine • Trimebutine • Rociverine • Dicycloverine • Dihexyverine • Difemerine • Piperidolate

Quaternary ammonium
compounds

Benzilone • Mepenzolate • Pipenzolate • Glycopyrronium • Oxyphenonium • Penthienate • Methantheline • Propantheline • Otilonium bromide • Tridihexethyl • Isopropamide • Hexocyclium • Poldine • Bevonium • Diphemanil • Tiemonium iodide • Prifinium bromide • Timepidium bromide • Fenpiverinium

Phosphodiesterase inhibitors

Papaverine • Drotaverine • Moxaverine

Acting on serotonin receptors

5-HT₃ antagonists (Alosetron, Cilansetron) • 5-HT₄ agonists (Mosapride, Prucalopride, Tegaserod)

Other

Fenpiprane • Diisopromine • Chlorbenzoxamine • Pinaverium • Fenoverine • Idanpramine • Proxazole • Alverine • Trepibutone • Isometheptene • Caroverine • Phloroglucinol • Silicones • Trimethyldiphenylpropylamine

Belladonna and derivatives
(antimuscarinics)

tertiary amines: Atropine • Hyoscyamine
quaternary ammonium compounds: Scopolamine (Butylscopolamine, Methylscopolamine) • Methylatropine • Fentonium • Cimetropium bromide

Propulsives
primarily dopamine antagonists (Metoclopramide/Bromopride, Clebopride, Domperidone, Alizapride) • 5-HT₄ agonists (Cinitapride • Cisapride)

M: DIG

anat(t, g, p)/phys/devp/enzy

noco/cong/tumr, sysi/epon

proc, drug(A2A/2B/3/4/5/6/7/14/16), blte

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