"目录号: HY-13720A

GPCR/G ProteinNeuronal Signaling-

Pergolide甲磺酸盐是有抗帕金森病特性的多巴胺受体激动剂。

Dopamine Receptor

相关产品

Chlorpromazine hydrochloride-Brexpiprazole-Haloperidol-Cabergoline-Clozapine-Cariprazine hydrochloride-L-DOPA-Perphenazine-Dopamine hydrochloride-Oxidopamine hydrobromide-Sertindole-B-HT 920-Azaperone-Fluphenazine dihydrochloride-Iloperidone-

生物活性

Description

Pergolide Mesylate is an antiparkinsonian agent which functions as a dopaminergic agonist.Target: Dopamine ReceptorPergolide mesylate (trade name Permax) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Pergolide mesylate functions as an agonist at the dopamine D2, D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline [1, 2]. Pergolide mesylate decreases plasma prolactin concentrations [3]. The weak agonist activity of pergolide at D1 receptors somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease. The drug is in decreasing use, as it is reported to be associated with a form of heart disease called cardiac fibrosis. The use of pergolide or cabergoline is associated with a significantly increased risk of newly diagnosed cardiac-valve regurgitation [4].

Clinical Trial

NCT01066403

Heidelberg University-Stanley Medical Research Institute

Schizophrenia

October 2003

NCT00624741

Valeant Pharmaceuticals International, Inc.

Parkinson Disease

NCT00000269

National Institute on Drug Abuse (NIDA)-New York State Psychiatric Institute

Cocaine-Related Disorders-Substance-Related Disorders

October 1995

Phase 2

NCT00252044

Bronx VA Medical Center

Schizotypal Personality Disorder-Other Personality Disorders

October 2000

NCT00197483

Hamamatsu University

Schizophrenia-Negative Symptoms-Cognitive Impairments

March 2003

Phase 2

NCT00000248

Medical University of South Carolina-National Institute on Drug Abuse (NIDA)

Cocaine-Related Disorders

February 1996

Phase 3

NCT00004433

Children's Hospital Medical Center, Cincinnati-FDA Office of Orphan Products Development

Tourette Syndrome

December 1994

NCT00000215

National Institute on Drug Abuse (NIDA)-Columbia University

Cocaine-Related Disorders

Phase 2

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References

[1].Lemberger, L. and R.E. Crabtree, Pharmacologic effects in man of a potent, long-acting dopamine receptor agonist. Science, 1979. 205(4411): p. 1151-3.

[2].Koller, W.C., et al., The pharmacological evaluation of pergolide mesylate as a potential anti-parkinson agent. Neuropharmacology, 1980. 19(9): p. 831-7.

[3].Franks, S., et al., Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia. British medical journal (Clinical research ed.), 1983. 286(6372): p. 1177.

[4].Schade, R., et al., Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med, 2007. 356(1): p. 29-38.