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A redox cycling model for the action ofβ-adrenoceptor agonists

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Summary

A cyclic redox mechanism for the action ofβ-adrenoceptor agonists is proposed. It has the following features: a)β-adrenoceptor agonists act by ‘reductive activation’ of theβ-adrenoceptor (R); b) the redox state of R is reciprocally coupled to the redox state of the guanine nucleotide binding protein (G); c) binding of GTP to G reverses the agonist-induced alteration of the redox states of R and G; d) according to a specific version of the model the activation process involves a disulfide-thiol interchange reaction which leads to a GTP-revertible cross-linking of R and G by a disulfide bond. The way in which desensitization events may interfere with the proposed redox cycle is discussed.

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  1. Friedrich Miescher-Institut, P.O. Box 2543, CH-4002, Basel, Switzerland

    P. W. Kühl

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Acknowledgments. The author thanks Dr D. Walz for a helpful discussion, Drs L. Birnbaumer and G. T. Robillard for critical reading of the manuscript and the Deutsche Forschungsgemeinschaft for financial support.

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Kühl, P.W. A redox cycling model for the action ofβ-adrenoceptor agonists. Experientia 41, 1118–1122 (1985). https://doi.org/10.1007/BF01951689

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