Search for Cholinolytic Agents with Selective Action on the Central Nervous System,
ARMY FOREIGN SCIENCE AND TECHNOLOGY CENTER CHARLOTTESVILLE VA
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Development of a method of distinguishing the effects of cholinolytics on the central and peripheral choline receptors, using the ability of cholinolytics to suppress the central and peripheral effects of arecoline in mice, is discussed. Certain analogs of amizyl differ in their blocking effects on the central and peripheral choline receptors by 22-34 times, demonstrating a selective effect on the central M-choline receptors. Indirect evidence is presented that the central and peripheral choline receptors differ in structure, since the activity of this series of compounds on each appears to depend on a certain optimum packing of alkyl groups around the amino groups, with different optimums for maximum effect on the central and peripheral choline receptors.