title: Species differences in the stereoselectivity of kappa opioid binding sites for [3H]U-69593 and [3H]ethylketocyclazocine.
abstract: Stereoselectivity of the binding sites for the specific kappa-opioid agonist [3H]U-69593, a benzeneacetamido based ligand was investigated in membrane suspension prepared from frog and rat brain, as well as guinea pig cerebellum, using the pure chiral forms of different unlabelled opiates. The ligand binding sites showed stereospecificity with at least three orders of magnitude differences in the affinities (measured as Ki values) of the opioid stereoisomer pairs both in rat and guinea pig membrane fractions. However, in frog brain membranes there was no substantial difference in potencies of the (-) and (+) isomers competing for the [3H]U-69593 binding sites. Another type of the kappa-site preferring opioid ligand, [3H]ethylketocyclazocine, a benzomorphan derivative was able to discriminate between (-) and (+) forms of the same compounds even in frog brain membrane preparation. Our data concerning binding profile of [3H]U-69593 in frog brain membranes are consistent with the observation that kappa opioid binding sites in frog (Rana esculenta) brain differ from those kappa-sites found in mammalian brains.
authors.affiliation: Institute of Biochemistry, Hungarian Academy of Sciences, Szeged.
authors.forename: S
authors.initials: S
authors.lastname: Benyhe
authors.forename: M
authors.initials: M
authors.lastname: Szücs
authors.forename: A
authors.initials: A
authors.lastname: Borsodi
authors.forename: M
authors.initials: M
authors.lastname: Wollemann
mesh_terms: D000818:Animals; D044482:Benzeneacetamides; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D016314:Ethylketocyclazocine / Q000378:metabolism*; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D011759:Pyrrolidines / Q000378:metabolism*; D011869:Radioligand Assay; D011893:Rana esculenta; D051381:Rats; D011919:Rats, Inbred Strains; D017473:Receptors, Opioid, kappa / Q000378:metabolism*; D012044:Regression Analysis; D013045:Species Specificity; D013237:Stereoisomerism
chemical_list: D044482:Benzeneacetamides; D011759:Pyrrolidines; D017473:Receptors, Opioid, kappa; D016314:Ethylketocyclazocine; C045444:U 69593