3H-mepyramine binding to histamine H1-receptors in guinea pig lung: Characteristics and regulation by ions |
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Authors: | M Lombroso S Nicosia |
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Institution: | Institute of Pharmacology and Pharmacognosy, University of Milan, Via A. Del Sarto 21, 20129 Milan, Italy |
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Abstract: | The antogonist 3H]-mepyramine is used to label histamine H1-receptors in guinea pig lung. Scatchard analysis reveals two classes of binding sites. Monovalent cations decrease steady-state binding (Na+ > Li+ > K+), while divalent cations (Mg++, Ca++, Mn++, Ba++) exhibit a biphasic curve, increasing binding at low concentrations and decreasing it at higher levels. Na+ decreases both affinity and number of binding sites. Dissociation curve shows two components, and Na+ accelerates the rate of dissociation of the slower component. GTP does not affect the binding of the antagonist 3H-Mepyramine. |
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