CHARACTERIZATION OF KAPPA-1 AND KAPPA-2 OPIOID BINDING-SITES IN FROG (RANA-ESCULENTA) BRAIN MEMBRANE PREPARATION

被引：39

作者：

BENYHE, S ^{[1
]}

VARGA, E ^{[1
]}

HEPP, J ^{[1
]}

MAGYAR, A ^{[1
]}

BORSODI, A ^{[1
]}

WOLLEMANN, M ^{[1
]}

机构：

[1] HUNGARIAN ACAD SCI,CENT RES INST CHEM,H-1025 BUDAPEST 17,HUNGARY

来源：

NEUROCHEMICAL RESEARCH | 1990年 / 15卷 / 09期

关键词：

[!sup]3[!/sup]H]ethylketocyclazocine; equibibrium binding experiments; frog brain; kappa receptors; Opioid receptor subtypes;

D O I：

10.1007/BF00965909

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The distribution and properties of frog brain kappa-opioid receptor subtypes differ not only from those of the guinea pig brain, but also from that of the rat brain. In guinea pig cerebellum the kappa1 is the dominat receptor subtype, frog brain contains mainly the kappa2 subtype, and the distribution of the rat brain subtypes is intermediate between the two others. In competition experiments it has been established that ethylketocyclazocine and N-cyclopropylmethyl-norazidomorphine, which are nonselective kappa-ligands, have relatively high affinities to frog brain membranes. The kappa2 ligands (Met5)enkephalin-Arg6-Phe7 and etorphine also show high affinities to the frog brain. Kappa1 binding sites measured in the presence of 5 μM /D-Ala2-Leu5/enkephalin represent 25-30% of [3H]ethylketocyclazocine binding in frog brain membranes. The kappa2 subtype in frog brain resembles more to the mu subtype than the delta subtype of opioid receptors, but it differs from the mu subtype in displaying low affinity toward beta-endorphin and /D-Ala2-(Me)Phe4-Gly5-ol/enkephalin (DAGO). From our data it is evident that the opioid receptor subtypes are already present in the amphibian brain but the differences among them are less pronounced than in mammalian brain. © 1990 Plenum Publishing Corporation.

引用

页码：899 / 904

页数：6

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