Intrinsic activity and effects of guanyl-5'-yl imidodiphosphate, Gpp(NH)p and sodium ion on the affinity of dynorphin 1-13, nalorphine and nalorphine-7,8-oxide to kappa-opioid receptor.
Nalorphine and nalorphine-7,8-oxide (nalorphine epoxide) behaved as partial agonists on the kappa-receptor in the electrically stimulated mouse vas deferens. The effects of a GTP-analogue, GppNHp and Na+ on the inhibition of [3H]ethylketocyclazocine binding by dynorphin 1-13, nalorphine, its epoxide and naloxone (antagonist) were studied with a synaptosomal fraction of guinea pig brain (except a cerebellum) and compared with the intrinsic activity of the test drugs, which was estimated in the electrically stimulated mouse vas deferens. The effects of GppNHp and Na+ on the affinity of the drugs to the kappa-receptor correlated with their intrinsic activities.
Takayanagi
I
I
Okumura
K
K
Konno
F
F
Koike
K
K
Cho
N
N
Hirobe
M
M
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D003496:Cyclazocine / Q000031:analogs & derivatives / Q000378:metabolism; D004399:Dynorphins / Q000037:antagonists & inhibitors; D016314:Ethylketocyclazocine; D006160:Guanosine Triphosphate / Q000031:analogs & derivatives*; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009269:Nalorphine / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors; D009270:Naloxone / Q000037:antagonists & inhibitors; D010446:Peptide Fragments / Q000037:antagonists & inhibitors; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects* / Q000378:metabolism; D017473:Receptors, Opioid, kappa; D012964:Sodium / Q000494:pharmacology*; D013574:Synaptosomes / Q000378:metabolism; D014649:Vas Deferens / Q000187:drug effects
D010446:Peptide Fragments; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D006165:Guanylyl Imidodiphosphate; D009270:Naloxone; D016314:Ethylketocyclazocine; C026843:dynorphin (1-13); D004399:Dynorphins; D006160:Guanosine Triphosphate; C047166:nalorphine-7,8-oxide; D012964:Sodium; D003496:Cyclazocine; D009269:Nalorphine