乳酸比哌立登

乳酸比哌立登用途

双哌啶(KL 373)乳酸是一种口服活性非选择性毒蕈碱受体拮抗剂,与M1毒蕈碱接收器竞争性结合。双哌啶(KL 373)乳酸抑制乙酰胆碱并增强中枢神经系统中的多巴胺信号。双哌啶(KL 373)乳酸对帕金森病和其他相关精神障碍的研究具有潜力[1][2]。

乳酸比哌立登名称

[ CAS 号 ]:
7085-45-2

[ 中文名 ]:
乳酸比哌立登

[ 英文名 ]:
biperiden lactate

乳酸比哌立登生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

研究领域 >> 神经疾病

[体外研究]

双肽乳酸(29.6μg/ml,72小时)在高剂量下可显著诱导人胰腺导管腺癌细胞凋亡和抑制增殖[1]。细胞增殖试验[1]细胞系：Panc-1、Panc-2和BxPC3人胰腺导管腺癌细胞浓度：29.6μg/mL孵育时间：72小时结果：通过减少核c-Rel易位,在72小时显著抑制细胞增殖。

[体内研究]

在使用Panc-1人胰腺导管腺癌细胞的皮下异种移植小鼠中,双肽乳酸(腹腔注射,10 mg/kg,每天,3周)将肿瘤大小减少83%。双哌啶乳酸(腹腔注射,8 mg/kg,每8小时,10天)可以减少自发癫痫发作的频率和细胞外海马谷氨酸水平,同时导致海马兴奋性的长期下降[2]。动物模型：用Panc-1人胰腺导管腺癌细胞皮下移植小鼠[1]剂量：10mg/kg给药：腹腔注射；每天的3周结果：肿瘤缩小83%。动物模型：雄性Wistar大鼠(200-250 g)[2]剂量：8 mg/kg给药：腹腔注射；每8小时；10天结果：在不影响情绪记忆损害的情况下,将迟发性癫痫发作减少约三倍

[参考文献]

[1]. Leonie Konczalla，et al. Biperiden and mepazine effectively inhibit MALT1 activity and tumor growth in pancreatic cancer. Int J Cancer. 2020 Mar 15;146(6):1618-1630.

[2]. Simone Bittencourt, et al. Modification of the natural progression of epileptogenesis by means of biperiden in the pilocarpine model of epilepsy. Epilepsy Res. 2017 Dec;138:88-97. doi: 10.1016/j.eplepsyres.2017.10.019. Epub 2017 Oct 29.

乳酸比哌立登物理化学性质

[ 沸点 ]:
462.1ºC at 760mmHg

[ 分子式 ]:
C₂₄H₃₅NO₄

[ 分子量 ]:
401.53900

[ 闪点 ]:
224.5ºC

[ 精确质量 ]:
401.25700

[ PSA ]:
81.00000

[ LogP ]:
3.35210

乳酸比哌立登毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OD5735000

CAS REGISTRY NUMBER :: 7085-45-2

LAST UPDATED :: 198710

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C21-H29-N-O.C3-H6-O3

MOLECULAR WEIGHT :: 401.60

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 161 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,74,1967

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 335 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,74,1967

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 61 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,74,1967