Document Report Card

ID: ALA1127058

Journal: J Med Chem

Title: The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.

Authors: Trybulski EJ, Zhang J, Kramss RH, Mangano RM.

Abstract: Previous pharmacological studies of methylated oxotremorine derivatives bearing substituents at the 3-, 4-, and 5-positions of the pyrrolidinone ring have been conducted using racemic mixtures, and not with optically active compounds. The synthesis and radioligand binding data of optically active, methylated oxotremorine derivatives at the 3- and 4-positions are described. There are significant pharmacological differences between the 3- and 4-position derivatives. The 4-position enantiomers have weak, approximately equal affinity and antagonist-like profiles, whereas the 3-position enantiomers have significantly different affinities and partial agonist-like profiles.

CiteXplore: 8246221

DOI: 10.1021/jm00075a007