- 英文名称
- Perospirone
- 分子式
- C23H30N4O2S
- 分子量
- 426.57
- 中文别名
- (3AS,7AR)-2-[4-[4-(1,2-苯并噻唑-3-基)哌嗪-1-基]丁基]-3A,4,5,6,7,7A-六氢异吲哚-1,3-二酮; rel-(3aR,7aS)-2-[4-[4-(1,2-苯并异噻唑-3-基)-1-哌嗪基]丁基]六氢-1H-异吲哚-1,3(2H)-二酮; 1H-Isoindole-1,3(2H)-dione, 2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-, (3aR,7aS)-rel- (9CI); 1H-Isoindole-1,3(2H)-dione, 2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-, cis-; cis-N-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cyclohexanedicarboximide; Perospirine; (3aR,7aS)-2-[4-[4-(1,2-benzothiazol-3-yl)-1-piperazinyl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione; (1R,2S)-N-[4-[4-(1,2-Benzisothiazole-3-yl)-1-piperazinyl]butyl]cyclohexane-1,2-dicarbimide; (3aR,7aS)-2-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione; Lullan; M813
- 用途
- - 哌罗匹隆（Perospirone），是一种白色粉末的化学品，为抗精神病药，临床上主要主料精神分裂症。
- 生物活性
Perospirone (SM-9018 free base) 是具有口服活性的 5-HT2A 受体 (Ki=0.6 nM) 和多巴胺 D2 受体 (Ki=1.4 nM) 的拮抗剂，也是 5-HT1A 受体 (Ki=2.9 nM) 的部分激动剂。Perospirone 是一种非典型的抗精神病剂，可用于精神分裂症的研究。
- 靶点
5-HT
2A
Receptor
0.6 nM (Ki)
Dopamine D
2
1.4 nM (Ki)
5-HT
1A
Receptor
2.9 nM (Ki)
5-HT
1
Receptor
18 nM (Ki)
Dopamine D
1
41 nM (Ki)
- 体外研究
Perospirone (SM-9018 free base) possesses moderate affinities for α
1
, 5-HT
1
, and D
1
receptors (K
i
=17, 18 and 41 nM, respectively) .
- 体内研究
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.
Animal Model:
Male ICR mice (6 weeks old) weighing 25-30 g
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.
