硫丙咪胺

生物活性靶点体外研究体内研究硫丙咪胺试剂级价格

硫丙咪胺

CAS号:106243-16-7
英文名:THIOPERAMIDE MALEATE
中文名:硫丙咪胺
CBNumber:CB5245732
分子式:C15H24N4S
分子量:292.44
MOL File:106243-16-7.mol

硫丙咪胺化学性质

储存条件 :Store at -20°C
溶解度 :H₂O: 10 mg/mL
形态 :solid
颜色 :white

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26-36
WGK Germany :3

硫丙咪胺性质、用途与生产工艺

生物活性 Thioperamide (MR-12842) 是一种有效的，具有口服活性的，可透过血脑屏障的选择性 H3 受体拮抗剂，抑制 [3H] 组胺释放的 Ki 为 4.3 nM。Thioperamide 抑制 [3H] 组胺合成的 Ki 为 31 nM 。
靶点

H ₃ Receptor

体外研究

Thioperamide inhibits [ ³ H]-(R)α-MeHA binding rat brain and guinea-pig lung with K _i s of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [ ³ H]histamine release with a mean apparent K _i of 4 nM.
Thioperamide (0.01-100 μM; 24 hours) promotes the viability of NE-4C stem cells in a concentration-dependent manner.

Cell Viability Assay

Cell Line:	NE-4C stem cells
Concentration:	0.01, 0.1, 1, 10, 100 μM
Incubation Time:	24 hours
Result:	The viability of NE-4C stem cells increased significantly to 150.83±6.91% when (1 μM) was administrated, and increased to 145.11±14.52% and 132.02%±25.65% when 10 μM and 100 μM were administrated respectively.

体内研究

Thioperamide (5-20 mg/kg; i.p.) is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice.

Animal Model:	Naive female C57BL/6J mice
Dosage:	5, 10 or 20 mg/kg
Administration:	Injections (i.p.)
Result:	Facilitated reconsolidation of a contextually-conditioned fear memory.