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Characterization of kappa1 and kappa2 opioid binding sites in frog (rana esculenta) brain membrane preparation

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Abstract

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.

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Abbreviations

DAGO:

/D-Ala2-(Me)Phe4-Gly5-ol/enkephalin

DALE:

/D-Ala2-L-Leu5/-enkephalin

EKC:

ethylketocyclazocine

DHM:

dihydromorphine

CAM:

N-cyclopropylmethylnorazidomorphine

nor-BNI:

nor-binaltorphimine

MR2034:

(-)-(1R,5R,9R)-5, 9-dimethyl-2 (L-tetrahydrofuryl-2'-hydroxy-6,7benzomorphan)

MR2035:

(+)-(1R,5R,9R)-5,9-dimethyl-2 (L-tetrahydrofuryl-2'-hydroxy-6,7-benzomorphan), U50488H=3,4-dichloro-N-/2-(1-pyrrolidinyl) —cyclohexo/-benzene-acetamide

PD117302:

trans-N-methyl-N-/2-(1-pyrrolidinyl) — cyclohexyl/-benzo (b) thiophene-4-acetamide

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Authors and Affiliations

  1. Institute of Biochemistry, Biological Research Center of Hungarian Academy of Sciences, P.O. Box 521, 6701, Szeged, Hungary

    Sandor Benyhe, Eva Varga, Anna Borsodi & Maria Wollemann

  2. Central Research Institute for Chemistry of Hungarian Academy of Sciences, P.O. Box 17, 1025, Budapest, Hungary

    Jozsef Hepp & Anna Magyar

Authors
  1. Sandor Benyhe
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  2. Eva Varga
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  3. Jozsef Hepp
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  4. Anna Magyar
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  5. Anna Borsodi
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  6. Maria Wollemann
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Benyhe, S., Varga, E., Hepp, J. et al. Characterization of kappa1 and kappa2 opioid binding sites in frog (rana esculenta) brain membrane preparation. Neurochem Res 15, 899–904 (1990). https://doi.org/10.1007/BF00965909

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