Adrenergic ligand liposolubility in membranes. Direct assessment in a beta-adrenergic binding system

The binding of [3H]dihydroalprenolol to adipocyte membranes may be displaced not only from beta-adrenergic receptors but also nonstereospecifically from other membrane compartments by beta-adrenergic and other adrenergic agents. The EC50 of this nonstereospecific displaceable binding is directly rel...

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Veröffentlicht in:	Molecular pharmacology 1982-07, Vol.22 (1), p.5-7
Hauptverfasser:	Dax, E M, Partilla, J S
Format:	Artikel
Sprache:	eng
Schlagworte:	adipocytes Adipose Tissue - metabolism Animals beta -adrenergic Binding, Competitive Dihydroalprenolol Isoproterenol - metabolism Ligands Membrane Lipids Membranes - metabolism Receptors, Adrenergic - metabolism Receptors, Adrenergic, beta - metabolism Solubility Sympathomimetics - metabolism
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Zusammenfassung:	The binding of [3H]dihydroalprenolol to adipocyte membranes may be displaced not only from beta-adrenergic receptors but also nonstereospecifically from other membrane compartments by beta-adrenergic and other adrenergic agents. The EC50 of this nonstereospecific displaceable binding is directly related to the liposolubility (n-octanol:water partition coefficient) of the displacing ligand.
ISSN:	0026-895X 1521-0111