Structural Determinants of Muscarinic Agonist Activity

Traditionally, structure-activity relationships (SAR) among muscarinic cholinergic agonists have been derived from dose-effect studies on isolated tissues or in whole animals (Barlow, 1964). In general, in vitro assays are preferable to in vivo assays for studying relations between chemical structure and actual effect (pharmacodynamics). The interpretation of SAR obtained in vivo is likely to be complicated by distributional and pharmacokinetic factors.