Novel phenylpiperidine opioid antagonists and partial agonists: effects on fluid consumption

• Published in: European journal of pharmacology Vol. 81; no. 2; p. 185
• Main Authors: Leander, J D, Hart, J C, Lochner, M A, Hynes, 3rd, M D, Zimmerman, D M
• Format: Journal Article
• Language: English
• Published: Netherlands 09-07-1982
• Subjects: Animals; Dose-Response Relationship, Drug; Drinking - drug effects; Male; Narcotic Antagonists - pharmacology; Narcotics - pharmacology; Piperidines - pharmacology; Radioligand Assay; Rats; Rats, Inbred Strains; Receptors, Opioid - metabolism; Stereoisomerism
• ISSN: 0014-2999
• DOI: 10.1016/0014-2999(82)90436-8

The effects of five opioid antagonists, a racemate partial agonist and its agonist and antagonist optical isomers were studied on deprivation-induced drinking. All compounds had a phenylpiperidine nucleus. The antagonists produced dose-related decreases in drinking, and the potencies for decreasing drinking correlated with morphine-antagonist doses. The racemic partial agonist and its agonist isomer decreased drinking at doses higher than those which produced marked analgesia. Within the class of phenylpiperidine drugs studied, some had less specificity than naloxone for the mu-receptors as compared to the delta-receptor, but the suppression of drinking was not related to changes in mu-to-delta ratios.