Milameline hydrochloride is a muscarinic receptor agonist that displays roughly equal affinity at all receptor subtypes (Ki values are 2.3, 2.4, 3.6, 3.8 and 4.3 μM for mAChR M1, mAChR M2, mAChR M3, mAChR M4, mAChR M5 (hM1, hM2, hM3, hM4 and hM5 receptors) respectively). Cognitive enhancer; reverses spatial memory deficits in rats.
Sedman et al (1995) Preclinical and phase I clinical characterization of CI-979/RU35926, a novel muscarinic agonist for the treatment of Alzheimer's disease. Life Sci. 56 877. Wood et al (1999) Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry. Br.J.Pharmacol. 126 1620. Schwarz et al (1999) Milameline (CI-979/RU35926): a muscarinic receptor agonist with cognition-activating properties: biochemical and in vivo characterization. J.Pharmacol.Exp.Ther. 291 812.
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