Binding profile of SM-9018, a novel antipsychotic candidate.
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.
Kato
T
T
Research Laboratories, Sumitomo Pharmaceuticals, Co., Ltd., Osaka, Japan.
Hirose
A
A
Ohno
Y
Y
Shimizu
H
H
Tanaka
H
H
Nakamura
M
M
D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism*; D001921:Brain / Q000378:metabolism*; D018492:Dopamine Antagonists; D007211:Indoles / Q000378:metabolism*; D054833:Isoindoles; D008297:Male; D008566:Membranes / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin / Q000378:metabolism; D013844:Thiazoles / Q000378:metabolism*
D014150:Antipsychotic Agents; D018492:Dopamine Antagonists; D007211:Indoles; D054833:Isoindoles; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D013844:Thiazoles; C065533:perospirone