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H1-receptor reserves in guinea-pig left atria, trachea and pig coronary artery as identified by phenoxybenzamine

  • Allery, Histamine and Kinins
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Abstract

H1-receptor reserves in guinea-pig left atria, trachea and pig coronary arteries were calculated by the use of phenoxybenzamine (Pba), a β-haloalkylamine that irreversibly blocks the H1-receptor response to histamine or 2-(2-pyridyl)-ethylamine (PEA). Equieffective concentrations of the H1-agonist in the absence (A) and presence (A′) of Pba were evaluated from concentration-response curves. By plotting the reciprocal values 1/A versus 1/A′ the amount of H1-receptors not occupied by the agonist was calculated. The size of the H1-receptor reserve could be estimated by comparison of the receptor occupation with the corresponding effect. Furthermore, the dissociation constants for histamine, PEA, Pba and the pD′2-values for Pba were determined for the different tissues. 5% and 6% H1-receptor occupation is necessary to achieve a half maximal contraction of the trachea with the agonists histamine and PEA, respectively. Only 0.5% H1-receptor occupation is needed for the half maximal positiv inotropic effect of histamine in left atria, while 5.5% of the H1-receptors have to be accupied using PEA as an agonist in this tissue. In the coronary artery of the pig 50% of the maximal contraction can be achieved by stimulation of 15.1% of the H1-receptors with histamine.

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Authors and Affiliations

  1. Institute of Pharmacology, University of Düsseldorf, Moorenstr. 5, D-4000, Düsseldorf, FRG

    E. Rappen-Cremer,  U. Borchard, D. Hafner & F. Berger

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  1. E. Rappen-Cremer
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  2. U. Borchard
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  3. D. Hafner
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  4. F. Berger
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Rappen-Cremer, E., Borchard, U., Hafner, D. et al. H1-receptor reserves in guinea-pig left atria, trachea and pig coronary artery as identified by phenoxybenzamine. Agents and Actions 28, 218–223 (1989). https://doi.org/10.1007/BF01967405

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  • DOI: https://doi.org/10.1007/BF01967405

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