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Allosteric Drugs Acting at Muscarinic Acetylcholine Receptors

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Abstract

The binding properties of muscarinic acetylcholine receptors are affected by various drugs acting at a second (allosteric) binding site, usually (but not always) at supratherapeutic concentrations. Allosteric drugs acting at GABA receptors present advantages over competitive drugs; this explains the interest raised by allosteric effects on muscarinic receptors. A theoretical and practicable definition of allosteric drugs acting at muscarinic receptors will be given in this work, together with a summary of recent data concerning the number, position, and structural requirements of their binding sites.

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  1. Department of Biochemistry and Nutrition, School of Medicine, Université Libre de Bruxelles, Bât G/E, CP 611, 808 Route de Lennik, B-1070, Bruxelles, Belgium

    Magali Waelbroeck

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Waelbroeck, M. Allosteric Drugs Acting at Muscarinic Acetylcholine Receptors. Neurochem Res 28, 419–422 (2003). https://doi.org/10.1023/A:1022888332221

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