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  • Title: Labelling of non-H1-receptor binding sites by [3H]-mepyramine on the rat liver plasma membrane.
    Author: Leurs R, Bast A, Timmerman H.
    Journal: Agents Actions; 1990 Apr; 30(1-2):157-60. PubMed ID: 2371917.
    Abstract:
    In the present study we characterized [3H]-mepyramine binding to rat liver plasma membranes. Binding of [3H]-mepyramine proved to be of high affinity (Kd = 7.7 +/- 0.4 nM) and saturable, resulting in a Bmax-value of 70.4 +/- 9.5 pmol/mg protein. However, displacement studies revealed that this binding site was different from other H1-receptor systems. The two stereoisomers of chlorpheniramine were rather ineffective in displacing [3H]-mepyramine and showed a stereospecificity in favour of the L-isomer. Also several H1-receptor agonists were not potent in displacing [3H]-mepyramine from rat liver plasma membranes. Moreover, the histamine metabolite imidazole-4-acetic acid was about as potent as the H1-agonists, whereas imidazole was even more potent. These data strongly suggest that [3H]-mepyramine labels a non-H1-receptor binding site on the rat liver plasma membrane.
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