106243-16-7
106243-16-7 结构式
基本信息
中文别名
硫丙咪胺 英文别名
ThiopMR 12842
thioperamide
THIOPERAMIDE MALEATE
THIOPERAMIDE MALEATE SALT
THIOPERAMIDE MALEATE (MR 12842) POTENT A ND SELECTIVE
N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide
N-Cyclohexyl-4-(1H-imidazol-4-yl)-1-piperidinecarbothioamide
N-CYCLOHEXYL-4-(1H-IMIDAZOL-5-YL)-1-PIPERIDINECARBOTHIOAMIDE
N-Cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide
常见问题列表
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. |