Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.

@article{Garvey1992SynthesisAI,
  title={Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.},
  author={David S. Garvey and J T Wasicak and John Y L Chung and Y K Shue and Gonçalo V. S. M. Carrera and Paul D. F. May and Martha M McKinney and Dirk Anderson and Ed C. Cadman and L Vella-Rountree},
  journal={Journal of medicinal chemistry},
  year={1992},
  volume={35 9},
  pages={1550-7}
}
A series of novel 2-substituted acetylenic pyrrolidines and piperidines related to oxotremorine (1) were prepared and evaluated in vitro as muscarinic cholinergic agents at brain M1 and M2 receptors. One analogue, 3-(2-oxo-1-pyrrolidinyl)-1-[2(R)-pyrrolidinyl]-1-propyne hydrogen oxalate (6a), was found to be a partial agonist producing a PI hydrolysis response at cortical M1 receptors approximately 3-fold larger than that produced by 1. The intrinsic activity profile of 6a at brain muscarinic… CONTINUE READING