The interactions of 1-alkyl-4,4-diphenylpiperidines with opiate receptors.
1-Alkyl-4,4-diphenylpiperidines inhibit the binding of mu- and delta-opiate receptor agonists to crude synaptosomal membranes of rat brain. Opiate receptor affinity is dependent on the nature of the 1-alkyl substitution. In displacing [3H]etorphine, [3H]dihydromorphine and [3H][D-Ala2,D-Leu5] enkephalin, the 1-methyl-derivative was most effective (IC50 [3H]etorphine = 9 microM, IC50 [3H]dihydromorphine = 0.71 microM, IC50 [3H][D-Ala2,D-Leu5]enkephalin = 2.1 microM). 1-t-Butyl-4,4-diphenylpiperidine and its 1-isopropyl analogue, used as antiparkinsonism drugs, exhibit distinctly lower inhibiting concentration values (50% inhibition, IC50 values).
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D066298:In Vitro Techniques; D008566:Membranes / Q000378:metabolism; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects*; D013574:Synaptosomes / Q000378:metabolism
D010880:Piperidines; D011957:Receptors, Opioid