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  • Title: Characteristics of [3H]mepyramine binding in DDT1MF-2 cells: evidence for high affinity binding to a functional histamine H1 receptor.
    Author: Dickenson JM, Hill SJ.
    Journal: Eur J Pharmacol; 1994 Jul 15; 268(2):257-62. PubMed ID: 7957647.
    Abstract:
    The binding characteristics of [3H]mepyramine to histamine H1 receptors in the smooth muscle cell line, DDT1MF-2, have been investigated. Competition binding experiments produced dissociation constants (Ki) for mepyramine, (+)-chlorpheniramine, and promethazine of 3.4 nM, 2.6 nM and 0.66 nM, respectively. Saturation binding using [3H]mepyramine produced a Kd of 2.1 nM and a Bmax of 47 fmol/mg protein. These data suggest that a high-affinity [3H]mepyramine binding site can be detected with the characteristics of the "classical" histamine H1 receptor. The low-affinity [3H]mepyramine binding site reported previously [Mitsuhashi, M. and Payan, D.G. (1988) J. Cell. Physiol. 134, 367-375] is predominantly to a secondary [3H]mepyramine site. The "low affinity" or secondary [3H]mepyramine binding site on DDT1MF-2 cells is insensitive to quinine (10 microM) and is therefore distinct from the [3H]mepyramine binding protein found in rat liver.
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