Activity of N-ethyl-nor-arecaidine Propargyl Ester and (R)-nipecotic Acid Ethyl Ester at Pre- and Postsynaptic Muscarinic Receptor Subtypes
The muscarinic activities of the heterocyclic acetylcholine analogues, N-ethyl-nor-arecaidine propargyl ester (NEN-APE), (R)- and (S)-nipecotic acid ethyl ester (NAEE) and guvacine propargyl ester (GPE), were determined at presynaptic M1- and postsynaptic M2- and M3-receptors using functional in vitro methods.
Abstract : We are interested in studying the muscarinic acetylcholine receptor. Our work will involve molecular modeling of muscarinic agonists and antagonists to determine their bioactive conformations. From the modeled ligands we hope to derive a pharmacophoric pattern common to the ligands. This pharmacophoric pattern will enable a topography of the muscarinic receptor to be derived which will facilitate the design of novel agonists and antagonists. The work will concentrate on the design of new antagonists which could be synthesized and tested by army collaborators. These antagonists we hope will prove to be new antidotes for organophosphate poisons. Keywords: Molecular structure; Molecule molecule interactions; Synthesis (Chemistry); Computer programs.