Interactions of N-cyclopropylmethyl(-)-6 beta-acetylthionormorphine with mu-, kappa-, delta- and sigma-opioid receptors.
1. Affinities of N-cyclopropylmethyl(-)-6 beta-acetylthionormorphine (KT-90) to mu-, kappa-, delta- and sigma-receptors were tested in rat brain membrane fractions using radioligand-receptor assays. 2. Though KT-90 had nonselectively high affinities to mu-, kappa- and delta-receptors, affinity of KT-90 to sigma-receptors was lower than those to the other three receptors. 3. Affinity of KT-90 to sigma-receptors was 1000 times lower than that of buprenorphine.
Takayanagi
I
I
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Koike
K
K
Satoh
M
M
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002047:Buprenorphine / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009022:Morphine Derivatives / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects*; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D017480:Receptors, sigma
D009022:Morphine Derivatives; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D017480:Receptors, sigma; C065295:KT 90; D002047:Buprenorphine