Solubilization of histamine H-1, GABA and benzodiazepine receptors

Moshe Gavish, Raymond S L Chang, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

Binding sites for histamine H-1, GABA and benzodiazepine receptors have been solubilized from mammalian brain membranes using, as detergents, digitonin for benzodiazepine and H-1 receptors and lysolecithin for GABA receptors. The dissociation constants for 3H-mepyramine at histamine H-1 (1.5 nM), 3H-muscimol at GABA (7 nM, 24 nM) and 3H-flunitrazepam at benzodiazepine receptors (1.5 nM) are similar to values in membrane preparations. The relative and absolute potencies of various drugs in competing for 3H-ligand binding to the three receptors are closely similar in the soluble and membrane bound states, indicating that the conformation of the receptor recognition site is maintained during solubilization. Maximal numbers of binding sites are about 50% of corresponding levels in the membrane bound state.

Original languageEnglish (US)
Pages (from-to)783-789
Number of pages7
JournalLife Sciences
Volume25
Issue number9
DOIs
StatePublished - Aug 27 1979

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GABA-A Receptors
Histamine
Membranes
Pyrilamine
Flunitrazepam
Histamine Receptors
Digitonin
Muscimol
Lysophosphatidylcholines
GABA Receptors
Benzodiazepines
Detergents
gamma-Aminobutyric Acid
Conformations
Brain
Binding Sites
Ligands
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Pharmacology

Cite this

Solubilization of histamine H-1, GABA and benzodiazepine receptors. / Gavish, Moshe; Chang, Raymond S L; Snyder, Solomon H.

In: Life Sciences, Vol. 25, No. 9, 27.08.1979, p. 783-789.

Research output: Contribution to journalArticle

Gavish, Moshe ; Chang, Raymond S L ; Snyder, Solomon H. / Solubilization of histamine H-1, GABA and benzodiazepine receptors. In: Life Sciences. 1979 ; Vol. 25, No. 9. pp. 783-789.
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