Selective protection of benzomorphan binding sites against inactivation by N-ethylmaleimide. Evidence for κ-opioid receptors in frog brain

J. Zawilska, A. Lajtha, A. Borsodi

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

Selective binding of [3H]bremazocine and [3H]-ethylketocyclazocine to κ-opioid receptor sites in frog (Rana esculenta) brain membranes is irreversibly inactivated by the sulfhydryl group alkylating agent N-ethylmaleimide (NEM). Pretreatment of the membranes with κ-selective compounds [ethylketocyclazocine (EKC), dynorphin (1-13), or U-50,488H] but not with [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DAGO; μ specific ligand) or [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DADLE; δ specific ligand) strongly protects the binding of the radioligands against NEM inactivation. These results provide more evidence for the existence of κ-opioid receptors in frog brain. The relatively high concentrations of NEM that are needed to decrease the specific binding of [3H]bremazocine together with the observation of an almost complete protection of its binding sites by NaCl suggest that bremazocine may act as an opioid antagonist in frog brain.

Original languageEnglish
Pages (from-to)736-739
Number of pages4
JournalJournal of Neurochemistry
Volume51
Issue number3
Publication statusPublished - 1988

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Benzomorphans
Ethylmaleimide
Opioid Receptors
Ethylketocyclazocine
Anura
Brain
Enkephalins
Binding Sites
Leucine-2-Alanine Enkephalin
(trans)-Isomer 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide
Rana esculenta
Ala(2)-MePhe(4)-Gly(5)-enkephalin
Ligands
Membranes
Narcotic Antagonists
Alkylating Agents
Observation
bremazocine

ASJC Scopus subject areas

  • Biochemistry
  • Cellular and Molecular Neuroscience

Cite this

Selective protection of benzomorphan binding sites against inactivation by N-ethylmaleimide. Evidence for κ-opioid receptors in frog brain. / Zawilska, J.; Lajtha, A.; Borsodi, A.

In: Journal of Neurochemistry, Vol. 51, No. 3, 1988, p. 736-739.

Research output: Contribution to journalArticle

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