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Labelling of non-H1-receptor binding sites by [3H]-mepyramine on the rat liver plasma membrane

  • Histamine Receptors and Antihistamines
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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 (K d =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 stercospecificity in favour of thel-isomer. Also several H1-receptor agonists were not potent in displacing [3H]-mepyramine from rat liver plasma membranes. Morcover, 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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Authors and Affiliations

  1. Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, de Boclelaan 1083, 1081 HV, Amsterdam, The Netherlands

    R. Leurs, A. Bast & H. Timmerman

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  1. R. Leurs
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  2. A. Bast
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  3. H. Timmerman
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Leurs, R., Bast, A. & Timmerman, H. Labelling of non-H1-receptor binding sites by [3H]-mepyramine on the rat liver plasma membrane. Agents and Actions 30, 157–160 (1990). https://doi.org/10.1007/BF01969026

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