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perospirone

Names

[ CAS No. ]:
150915-41-6

[ Name ]:
perospirone

[Synonym ]:
(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

Biological Activity

[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.

Chemical & Physical Properties

[ 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

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds