U-32,802A is an

antipsychotic Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), p ...

tranquilizer A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are central nervous system (CNS) depressants and interact with brain activity, causing its deceleration. Various kinds of sedatives c ...

of the

butyrophenone Butyrophenone is an organic compound with the formula C6H5C(O)C3H7. It is a colorless liquid. The butyrophenone structure—a ketone flanked by a phenyl ring and a butyl chain—forms the basis for many other chemicals containing various subst ...

class. It was developed by Daniel Lednicer at

Upjohn The Upjohn Company was an American pharmaceutical manufacturing firm (est. 1886) in Hastings, Michigan, by Dr. William E. Upjohn, an 1875 graduate of the University of Michigan medical school. The company was originally formed to make ''friable ...

Pharmaceuticals in the early part of the 1970’s. Whereas related agents are based on a 4-aryl-

piperidine Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor de ...

central ring system, U-32,802A is an 4-aryl-

cyclohexylamine Cyclohexylamine is an organic compound, belonging to the aliphatic amine class. It is a colorless liquid, although, like many amines, samples are often colored due to contaminants. It has a fishy odor and is miscible with water. Like other amines, ...

, which might be expected to offer a unique pharmacological profile. Based on the available pharmacological data, U-32,802A was hypothesized to act primarily at the

presynaptic In the nervous system, a synapse is a structure that allows a neuron (or nerve cell) to pass an electrical or chemical signal to another neuron or a target effector cell. Synapses can be classified as either chemical or electrical, depending o ...

organelles for storage of monoamines in a way similar to

tetrabenazine Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorders. It is sold under the brand names Nitoman and Xenazine among others. On August 15, 2008, the US Food and Drug Administration (FDA) approved the use of tet ...

Analogs

Cyclohexylamine butyrophenones

A large number of cyclohexylamine butyrophenones was reported by Lednicer et al.: # PC12251406 # PC83261250 4-(2-Methoxyphenyl)cyclohex-3-en-1-amine, #PC37529 # Benzospirans: # 2-amino-5-phenylbicyclo .3.1onanes # PC12230284

4-Arylcyclohexylamines

All four of these designs are also antipsychotics, but they differ in that they were patented by companys other than for Lednicer and employ a different variety of sidechain than was seen above for the butyrophenones. Interestingly, although PC15079631 was listed as an antipsychotic, its mode of auction was to augment dopaminergic neurotransmission and not to inhibit it. This paradoxical mode of antipsychotic action was likewise reported for PD137789 & for PD-158771 # Pramiverine is an antispasmodic. # SIR 117 1695-51-6is an antidepressant.

References

{{Dopamine receptor modulators Butyrophenone antipsychotics 4-Fluorophenyl compounds Cyclohexenes