SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL PROFILE OF TROPICAMIDE ENANTIOMERS

The synthesis, chemical characterization and antimuscarinic activity o f the two enantiomers of tropicamide are reported. Functional (rabbit vas deferens, guinea pig heart (force) and ileum) as well as binding e xperiments (m(1) and m(4) human muscarinic receptors expressed in CHO- K1 cells; M(2) and M(3) receptors of rat heart and submaxillary gland membranes) were used to evaluate the antimuscarinic activity of the en antiomers. The results show that none of the enantiomers is able to si gnificantly discriminate among the receptors studied and therefore do not support the proposal of tropicamide as an M(4) (m(4)) selective ag ent.