7182. Perospirone

Nomenclature

CAS number: 150915-41-6
(3aR,7aS)-rel-2-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-1H-isoindole-1,3(2H)-dione; cis-N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cyclohexanedicarboximide.
C23H30N4O2S; mol wt 426.57.
C 64.76%, H 7.09%, N 13.13%, O 7.50%, S 7.52%.

Description and references

Serotonin (5-HT2) and dopamine (D2) antagonist (SDA). Prepn (stereochem unspec): K. Ishizumi et al., EP 196096; eidem, US 4745117 (1986, 1988 both to Sumitomo). Prepn of cis-form: eidem, Chem. Pharm. Bull. 43, 2139 (1995). Receptor binding profile in rat brain: T. Kato et al., Jpn. J. Pharmacol. 54, 478 (1990). Pharmacology: H. Sakamoto et al., Pharmacol. Biochem. Behav. 60, 873 (1998). Clinical trial in schizophrenia: M. Murasaki et al., Clin. Eval. 24, 159 (1997). Review of pharmacological profile: Y. Ohno et al., Pol. J. Pharmacol. 49, 213-219 (1997); and clinical experience: S. V. Onrust, K. McClellan, CNS Drugs 15, 329-337 (2001).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 129273-38-7
SM-9018; Lullan (Sumitomo).
C23H30N4O2S.HCl; mol wt 463.04.
C 59.66%, H 6.75%, N 12.10%, O 6.91%, S 6.92%, Cl 7.66%.

Properties

Prepd as dihydrate, mp 192-193°.

Therapeutic Category

Antipsychotic.

Keywords

Antipsychotic; Serotonin-Dopamine Antagonist