Quinpirole hydrochloride, a potential anti-parkinsonism drug.
Quinpirole hydrochloride, a putative dopamine agonist, was investigated in animal models of central dopaminergic activity, to evaluate its possible role in the treatment of Parkinson's disease. The drug induced stereotyped sniffing in rats but, unlike apomorphine, did not produce a maximal behavioural response (stereotyped gnawing). Pretreatment with neuroleptics blocked the stereotypy induced by quinpirole. Quinpirole reversed the effects of reserpine and alpha-methyl-paratyrosine, caused dose-dependent contralateral rotations in rats with unilateral lesions of the substantia nigra induced by 6-hydroxydopamine and induced vomiting in dogs. Small doses of quinpirole decreased locomotor activity, an effect presumably mediated by pre-synaptic autoreceptors. Quinpirole bound to D2 dopamine receptors in the striatum of the rat. The chronic injection of both subthreshold and suprathreshold doses, failed to induce behavioral supersensitivity. These data indicate that quinpirole can stimulate central dopaminergic receptors, and that it is a partial agonist with direct-acting properties. Quinpirole differs from other dopaminergic drugs and may be useful for the therapy of Parkinson's disease.
Koller
W
W
Department of Neurology, Loyola Medical Center, Hines VA Hospital, Chicago, IL.
Herbster
G
G
Anderson
D
D
Wack
R
R
Gordon
J
J
D000818:Animals; D001552:Benzazepines / Q000494:pharmacology; D003342:Corpus Striatum / Q000378:metabolism; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004873:Ergolines / Q000627:therapeutic use*; D006120:Grooming / Q000187:drug effects; D006220:Haloperidol / Q000494:pharmacology; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D010300:Parkinson Disease / Q000188:drug therapy*; D019257:Quinpirole; D051381:Rats; D011919:Rats, Inbred Strains; D013134:Spiperone / Q000378:metabolism; D013239:Stereotyped Behavior / Q000187:drug effects; D013469:Sulpiride / Q000494:pharmacology
D001552:Benzazepines; D004873:Ergolines; D019257:Quinpirole; D013134:Spiperone; D013469:Sulpiride; D006220:Haloperidol