Spirovesamicols

Details Spirovesamicols Spirovesamicols

1993-10-05

1995-10-10

Chang, Celia

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546 19, 546 44, 546150, 546187, 546206, 546240, 546241, 544392, C07D21120

Patent

active

054572070

ABSTRACT:
The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein "spirovesamicols" which are spirofused piperidines. The compounds bind to the vesamicol receptor, a site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.

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patent: 3666764 (1972-05-01), Campbell
patent: 4593037 (1986-06-01), Sarges
patent: 4595535 (1986-06-01), Vlattas
patent: 5023266 (1991-06-01), Langer et al.
patent: 5219860 (1993-06-01), Chambers
patent: 5324733 (1994-06-01), Billington
"The Neuromuscular Blocking Action of 2-(4-Phenylpiperidino) Cyclohexanol (AH 5183)", Brittain et al. 1969.
"The Vesicular Acetylcholine Transport System", Marshall and Parsons, 1987.
"Fractional Vesamicol Receptor Occupancy and Acetylcholine Active Transport Inhibition in Synaptic Vesciles", Kaufman et al. 1988.
"Fractional Vesamicol Receptor Occupancy and Acetylcholine Active Transport Inhibition in Synaptic Vesicles", Kaufman 1988.
"Synthesis, In Vitro Acetylcholine-Storage-Blocking Activities, and Biological Properties of Derivatives and Anaogues of Trans-2-(4-Phenylpiperidino) Cyclohexanol (Vesamicol)", Rogers et al., 1989.
"Acyclic Analogues of 2-4(Phenylpiperidino)Cyclohexanol (Vesamicol): Conformationally Mobile Inhibtiors of Vesicular Acetycholine Transport", Efange et al. 1991.
"Antiphyshotic Agents", Carl Kaiser et al., Burger's Medicinal Chemistry, Fourth Edition, Part III. (1987).

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