Pharmacokinetic and pharmacodynamic evaluations of the zwitterionic metabolite of a new series of N-substituted soft anticholinergics.

Purpose: This study was conducted to evaluate the zwitterionic common metabolite of a novel series of N-substituted soft analogs of glycopyrrolate both as racemates and as 2R isomers.

Methods: Activities were assessed using both in vitro (receptor binding assay, guinea pig ileum pA2 assay) and in vivo techniques (rabbit mydriatic response, rat cardiac effects). Pharmacokinetic characterizations in rats were also performed.

Design, pharmacokinetic, and pharmacodynamic evaluation of a new class of soft anticholinergics.

Purpose: To design and evaluate a new class of soft anticholinergics with subtype selectivity.

Methods: A new class of soft anticholinergics was designed based on the "inactive metabolite" approach. Four compounds were synthesized.