Azavesamicols

Details Azavesamicols Azavesamicols

1993-09-17

1998-08-04

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

436 63, 436 96, 436805, A01N 4340, A61K 31445, G01N 3300

Patent

active

057894205

ABSTRACT:
The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein "azavesamicols" in which the cyclohexyl group of vesamicol is replaced with a heterocycle of similar size, the piperidyl ring. The compounds bind to the vesamicol receptor, a cytoplasmically-oriented site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.

REFERENCES:
patent: 5077035 (1991-12-01), Wieland et al.
Rogers et al., Synthesis, in Vitro Acetylcholine-Storage-Blocking Activities, and Biological Properties of Derivatives and Analogues of trans-2-(4-Phenylpiperidino) Cyclohexanol (Vesauicol), J. Med. Chem. vol. 32, 1989, pp. 1217-1230.

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