2-Phenyl-4-(aminomethyl)imidazoles as Potential Antipsychotic Agents. Synthesis and Dopamine D2 Receptor Binding

A series of 2-phenyl-4-(aminomethyl)imidazoles were designed as conformationally restricted analogs of the dopamine D2 selective benzamide antipsychotics. The title compounds were synthesized and tested for blockade of [3H]YM-09151 binding in cloned African green monkey dopamine D2 receptor preparat...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1995-06, Vol.38 (12), p.2251-2255
Main Authors: Thurkauf, Andrew, Hutchison, Alan, Peterson, John, Cornfield, Linda, Meade, Robin, Huston, Kevin, Harris, Kristine, Ross, Philip C, Gerber, Karen, Ramabhadran, T. V
Format: Article
Language:English
Subjects:
Animals
Antipsychotic Agents - chemical synthesis
Antipsychotic Agents - metabolism
Antipsychotic Agents - pharmacology
Biological and medical sciences
Catecholaminergic system
Cercopithecus aethiops
CHO Cells
Cloning, Molecular
Cricetinae
DNA, Complementary
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - metabolism
Imidazoles - pharmacology
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Protein Binding
Receptors, Dopamine D2 - drug effects
Receptors, Dopamine D2 - genetics
Receptors, Dopamine D2 - metabolism
Structure-Activity Relationship
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Summary:A series of 2-phenyl-4-(aminomethyl)imidazoles were designed as conformationally restricted analogs of the dopamine D2 selective benzamide antipsychotics. The title compounds were synthesized and tested for blockade of [3H]YM-09151 binding in cloned African green monkey dopamine D2 receptor preparations. The binding affinity data thus obtained were compared against that of the benzamides and a previously described series of 2-phenyl-5-(aminomethyl)-pyrroles.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00012a026