Allosteric drugs acting at muscarinic acetylcholine receptors.
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.
Waelbroeck
Magali
M
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. mawaelbr@ulb.ac.be
D000494:Allosteric Regulation; D000818:Animals; D008024:Ligands; D008954:Models, Biological; D011976:Receptors, Muscarinic / Q000378:metabolism*
D008024:Ligands; D011976:Receptors, Muscarinic