Interactions of some 4-anilinopiperidines and 4-phenylpiperidines with the mu, delta- and kappa-binding sites.
The binding and pharmacological profiles of some 4-anilinopiperidine and 4-phenylpiperidine analogues were determined. The potency of the compounds to displace the binding of selective tritiated ligands was measured in homogenates of guinea-pig brain at 25 degrees C. All the compounds tested had high affinity for the mu-binding site, low affinity for the delta-site and were almost inactive at the kappa-site. The compounds were also tested for agonist activity in the guinea-pig ileum and the vasa deferentia of the mouse and rat. The pharmacological and binding profiles were compared.
D000818:Animals; D001921:Brain / Q000378:metabolism*; D004745:Enkephalins / Q000378:metabolism; D006168:Guinea Pigs; D008297:Male; D010880:Piperidines / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu
D004745:Enkephalins; D010880:Piperidines; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu