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The behavioral pharmacology of Ay‐27,110, a novel nonergot dopaminergic agonist
Author(s) -
Voith Katherine
Publication year - 1984
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430040403
Subject(s) - lisuride , pergolide , stereotypy , pharmacology , bromocriptine , dopaminergic , apomorphine , dopamine agonist , agonist , chemistry , haloperidol , pimozide , dopamine , reserpine , endocrinology , medicine , prolactin , amphetamine , receptor , hormone
Abstract AY‐27,110 is the pharmacologically active enantiomer of a troponylpiperazine derivative. At low doses, the compound induced contralateral rotational behavior in rats with a unilateral 6‐OHDA lesion of the nigrostriatal pathway, at higher doses it caused weak stereotypy and in dogs in elicited emesis. The actions of AY‐27,110 were dose‐dependently antagonized by haloperidol and pimozide, but were not diminished by α‐MPT or reserpine pretreatment. These results indicate that AY‐27,110 is a chemically novel dopaminergic agonist that should be useful as an anti‐parkinson drug. Since the effects of AY‐27,110 are independent of intact catecholamine synthesis and storage mechanisms, the compound should be efficacious in patients with advanced Parkinson's disease. AY‐27,110 was compared to several ergot‐derived dopamine agonists, namely bromocriptine, lisuride, and pergolide, in order to predict its potency, side‐effect liability, and potential therapeutic advantages.