References of (3aR,7aS)-2-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-3a,4,5,6,
7,7a-hexahydroisoindole-1,3-dione
Title: Perospirone
CAS Registry Number: 150915-41-6
CAS Name: (3a
R,7a
S)-
rel-2-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-1
H-isoindole-1,3(2
H)-dione
Synonyms: cis-N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cyclohexanedicarboximide
Molecular Formula: C23H30N4O2S
Molecular Weight: 426.57
Percent Composition: C 64.76%, H 7.09%, N 13.13%, O 7.50%, S 7.52%
Literature 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).
Derivative Type: Hydrochloride
CAS Registry Number: 129273-38-7
Manufacturers' Codes: SM-9018
Trademarks: Lullan (Sumitomo)
Molecular Formula: C23H30N4O2S.HCl
Molecular Weight: 463.04
Percent Composition: 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°.
Melting point: mp 192-193°
Therap-Cat: Antipsychotic.
Keywords: Antipsychotic; Serotonin-Dopamine Antagonist.