Kappa-opioid agonist inhibits phospholipase C, possibly via an inhibition of G-protein activity.
In synaptic membranes of guinea pig cerebellum, in which preparations U-50, 488H, a kappa-opioid agonist inhibits G-protein activity, the same kappa-agonist at 100 nM inhibited the phospholipase C (PLC) activity stimulated by 100 microM GTP in the presence of 10 microM Ca2+. The present study provides a unique hypothetical mechanism that the receptor-mediated inhibition of PLC is mediated by inhibition of G-protein activity.
Misawa
H
H
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
Ueda
H
H
Satoh
M
M
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000818:Animals; D002531:Cerebellum / Q000187:drug effects / Q000378:metabolism*; D019204:GTP-Binding Proteins / Q000494:pharmacology*; D006168:Guinea Pigs; D008297:Male; D011759:Pyrrolidines / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000187:drug effects / Q000502:physiology*; D017473:Receptors, Opioid, kappa; D010738:Type C Phospholipases / Q000378:metabolism*
D011759:Pyrrolidines; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D010738:Type C Phospholipases; D019204:GTP-Binding Proteins