盐酸哌罗匹隆

盐酸哌罗匹隆用途

Perospirone hydrochloride (SM-9018) 是具有口服活性的 5-HT2A 受体 (Ki 为 0.6 nM) 和多巴胺 D2 受体 (Ki 为 1.4 nM) 的拮抗剂,也是 5-HT1A 受体 (Ki 为 2.9 nM) 的部分激动剂。Perospirone hydrochloride 是一种非典型的抗精神病剂,可用于精神分裂症的研究。

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盐酸哌罗匹隆名称

[ CAS 号 ]:
129273-38-7

[ 中文名 ]:
盐酸哌罗匹隆

[ 英文名 ]:
Perospirone hydrochloride

[中文别名 ]:

[英文别名 ]:

MFCD08457543
Perospirone hydrochloride

盐酸哌罗匹隆生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT2A Receptor:0.6 nM (Ki)

D2 Receptor:1.4 nM (Ki)

5-HT1A Receptor:2.9 nM (Ki)

5-HT1 Receptor:18 nM (Ki)

D1 Receptor:41 nM (Ki)

[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.

盐酸哌罗匹隆物理化学性质

[ 沸点 ]:
667.4ºC at 760 mmHg

[ 熔点 ]:
95-970ºC

[ 分子式 ]:
C₂₃H₃₁ClN₄O₂S

[ 分子量 ]:
463.036

[ 闪点 ]:
357.4ºC

[ 精确质量 ]:
462.185638

[ PSA ]:
84.99000

[ LogP ]:
4.11650

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
-20°C Freezer

盐酸哌罗匹隆毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NR3397915

CHEMICAL NAME :: 1H-Isoindole-1,3(2H)-dione, 2-(4-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl )hexahydro-, monohydrochloride, cis-

CAS REGISTRY NUMBER :: 129273-38-7

LAST UPDATED :: 199806

DATA ITEMS CITED :: 7

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 870 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 31,177,1997

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 33 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 31,177,1997

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 660 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 31,177,1997

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2 gm/kg

TOXIC EFFECTS :: Liver - fatty liver degeneration Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 31,201,1997 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9125 mg/kg/1Y-I

TOXIC EFFECTS :: Liver - other changes Endocrine - changes in adrenal weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 31,309,1997

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2275 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - tremor Endocrine - changes in thymus weight Blood - changes in leukocyte (WBC) count

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 31,201,1997

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 1820 mg/kg/52W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Behavioral - somnolence (general depressed activity) Behavioral - tremor

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 31,309,1997