"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.