150915-41-6

150915-41-6 structure

Name: perospirone
Chemical Name: (3aR,7aS)-2-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione
CAS Number: 150915-41-6
Molecular Formula: C₂₃H₃₀N₄O₂S
Molecular Weight: 440.602
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-03-27 08:00:00
Modify Date: 2024-01-02 01:33:13
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic drug and has the potential for schizophrenic disease[1][2].

Name	(3aR,7aS)-2-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione
Synonyms	(3aR,7aS)-2-{4-[4-(1H-2,3-Benzothiazin-4-yl)piperazin-1-yl]butyl}hexahydro-1H-isoindole-1,3(2H)-dione cis-N-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cyclohexanedicarboximide Lullan (3aR,7aS)-2-{4-[4-(1H-2,3-Benzothiazin-4-yl)-1-piperazinyl]butyl}hexahydro-1H-isoindole-1,3(2H)-dione 1H-Isoindole-1,3(2H)-dione, 2-[4-[4-(1H-2,3-benzothiazin-4-yl)-1-piperazinyl]butyl]hexahydro-, (3aR,7aS)- Perospirone M813 UNII-N303OK87DT

Description	Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic drug and has the potential for schizophrenic disease[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2A Receptor:0.6 nM (Ki) Dopamine D2:1.4 nM (Ki) 5-HT1A Receptor:2.9 nM (Ki) 5-HT1 Receptor:18 nM (Ki) Dopamine D1:41 nM (Ki)
In Vitro	Perospirone (SM-9018 free base) possesses moderate affinities for α1, 5-HT1, and D1 receptors (Ki=17, 18 and 41 nM, respectively) [1].
In Vivo	Perospirone (SM-9018 free base; 1.0-10.0 mg/kg/day; orally; for 14 consecutive days) significantly attenuates PCP-induced cognitive deficits in mice in a dose-dependent manner[2]. Animal Model: Male ICR mice (6 weeks old) weighing 25-30 g[2] Dosage: 1.0, 3.0 or 10.0 mg/kg Administration: Orally; daily; for 14 consecutive days Result: Significantly attenuated PCP-induced cognitive deficits in mice in a dose-dependent manner.
References	[1]. Kato T, et al. Binding profile of SM-9018, a novel antipsychotic candidate. pn J Pharmacol. 1990 Dec;54(4):478-81. [2]. Hagiwara H, et al. Phencyclidine-induced cognitive deficits in mice are improved by subsequent subchronic administration of the antipsychotic drug perospirone: role of serotonin 5-HT1A receptors. Eur Neuropsychopharmacol. 2008 Jun;18(6):448-54.

Density	1.4±0.1 g/cm3
Boiling Point	648.8±65.0 °C at 760 mmHg
Molecular Formula	C₂₃H₃₀N₄O₂S
Molecular Weight	440.602
Flash Point	346.2±34.3 °C
Exact Mass	440.224609
PSA	84.99000
LogP	1.85
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.702

7716-66-7

150915-41-6

Literature: Chemical and Pharmaceutical Bulletin, , vol. 43, # 12 p. 2139 - 2151

Precursor 1
7716-66-7
DownStream 0

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