TY - JOUR T1 - Muscarinic activity and receptor binding of the enantiomers of aceclidine and its methiodide. JF - Molecular Pharmacology JO - Mol Pharmacol SP - 594 LP - 599 VL - 21 IS - 3 AU - B Ringdahl AU - F J Ehler AU - D J Jenden Y1 - 1982/05/01 UR - http://molpharm.aspetjournals.org/content/21/3/594.abstract N2 - The agents (+)- and (-)-aceclidine (3-acetoxyquinuclidine), (+)- and (-)-N-methylaceclidine, and oxotremorine were compared in their ability to inhibit specific 3H-labeled (+/-)-3-quinuclidinyl benzilate binding to rat brain muscarinic receptors and to stimulate contractions of the isolated guinea pig ileum. A good correlation was observed between the high-affinity dissociation constant (KH) for binding and the muscarinic potency in the isolated ileum. The binding data for the enantiomers of aceclidine were also consistent with their central and peripheral pharmacological activity in vivo. Thus the enantiomeric potency ratios [ED50 of (-)-aceclidine/ED50 of (+)-aceclidine] for the tremorogenic, analgesic, and sialogogic effects in mice agreed well with the ratio KH of (-)-aceclidine/KH of (+)-aceclidine. ER -