Osemozotan hydrochloride

Osemozotan hydrochloride (MKC242) is a selective 5-HT1A receptor agonist. Osemozotan hydrochloride decreases the number of c-Fos-positive cells caused by MAMP in mice. Osemozotan hydrochloride can be used for the research of depressive disorder[1][2].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Osemozotan hydrochloride (1 mg/kg; i.p.; 20 min after picrotoxin treatment) ameliorates picrotoxin-induced decrease in female preference with the combination of (+)-SKF-10,047[1]. Osemozotan hydrochloride (1 mg/kg; i.p.; once) decreases the number of c-Fos-positive cells caused by MAMP[2]. Animal Model: Female CD-1 mice with picrotoxin-induced decrease in female preference[1] Dosage: 1 mg/kg Administration: Intraperitoneal injection; 1 mg/kg; 20 min after picrotoxin treatment Result: Ameliorated the picrotoxin-induced decrease in the female preference by co-administration WITH (+)-SKF-10,047 (5 mg/kg). Showed no effect on the picrotoxin-induced decrease in the female preference when treated alone. Animal Model: ICR mice with MAMP injection[2] Dosage: 1 mg/kg Administration: Intraperitoneal injection; 1 mg/kg; once Result: Significantly decreased the number of c-Fos-positive cells induced by MAMP in the medial prefrontal cortex and striatum, but did not change the number of c-Fos-positive cells.

[1]. Hasebe S, et al. Anti-anhedonic effect of selective serotonin reuptake inhibitors with affinity for sigma-1 receptors in picrotoxin-treated mice. Br J Pharmacol. 2017 Feb;174(4):314-327.  

[2]. Tsuchida R, et al. Inhibitory effects of osemozotan, a serotonin 1A-receptor agonist, on methamphetamine-induced c-Fos expression in prefrontal cortical neurons. Biol Pharm Bull. 2009 Apr;32(4):728-31.  

MOLECULAR FORMULA :

C19-H21-N-O5.Cl-H

MOLECULAR WEIGHT :

379.87

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

100 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #5168099