Perospirone (Synonyms: 哌罗匹隆; SM-9018 free base)
目录号: PL05401 纯度: ≥99%
CAS No. :150915-41-6
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中文名称
Perospirone
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;非奈西林;哌罗匹隆
英文名称
Perospirone
英文别名
1H-Isoindole-1,3(2H)-dione,2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-,(3aR,7aS)-rel-;1H-Isoindole-1,3(2H)-dione,2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-,(3...;PEROSPIRINE;[14C]-Perospirone;[3H]-Perospirone;AC1L3H05;CHEMBL1472975;cis-2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-hexahydro-1H-isoindole-1,3(2H)-dione;Lullan;M813;Perospirone;SureCN120579;UNII-N303OK87DT;PEROSPIRONE HCL;cis-N-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cyclohexanedicarboximide;(1R,2S)-N-[4-[4-(1,2-Benzisothiazole-3-yl)-1-piperazinyl]butyl]cyclohexane-1,2-dicarbimide;1H-Isoindole-1,3(2H)-dione, 2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-, cis-;(3aα,7aα)-2-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-1H-isoindole-1,3(2H)-dione;(3aS,7aR)-2-[4-[4-(1,2-Benzothiazol-3-Yl)Piperazin-1-Yl]Butyl]-3a,4,5,6,7,7a-Hexahydroisoindole-1,3-Dione;1H-Isoindole-1,3(2H)-dione, 2-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-, (3aR,7aS)-rel- (9CI)
Cas No.
150915-41-6
分子式
C23H30N4O2S
分子量
426.57
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT 2A receptor (K i =0.6 nM) and dopamine D 2 receptor (K i =1.4 nM), and also a partial agonist of 5-HT 1A receptor (K i =2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
性状
Solid
IC50 & Target[1][2]
5-HT2A Receptor 0.6 nM (Ki) Dopamine D2
体外研究(In Vitro)
Perospirone (SM-9018 free base) possesses moderate affinities for α1, 5-HT1, and D1 receptors (Ki=17, 18 and 41 nM, respectively) . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 5 mg/mL (11.72 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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