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Binding Profile of SM-9018, a Novel Antipsychotic Candidate
Author(s) -
Terufumi Kato,
Akira Hirose,
Yukihiro Ohno,
Hiroshi Shimizu,
Hiroyasu Tanaka,
Mitsutaka Nakamura
Publication year - 1990
Publication title -
the japanese journal of pharmacology
Language(s) - English
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.54.478
Subject(s) - receptor , gabaa receptor , opiate receptors , binding site , phencyclidine , chemistry , antipsychotic , biochemistry , antagonist , nmda receptor , medicine , schizophrenia (object oriented programming) , psychiatry , (+) naloxone
The present study employed various receptor-binding assays to clarify the biochemical characteristics of SM-9018. SM-9018 possessed very high affinity for 5-HT2, D2 and 5-HT1A receptors (Ki = 0.61, 1.4 and 2.9 nM, respectively), and it had moderate affinity for alpha 1 and D1 receptors (Ki = 17 and 41 nM, respectively). However, SM-9018 had only negligible affinity for alpha 2, opiate, glutamate, phencyclidine, benzodiazepine and GABAA receptors. These results suggest that SM-9018 may be a novel antipsychotic agent with binding affinity for 5-HT2 and 5-HT1A receptors.

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