106243-16-7
106243-16-7 結(jié)構(gòu)式
基本信息
中文別名
硫丙咪胺 英文別名
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
常見問題列表
生物活性
Thioperamide (MR-12842) 是一種有效的，具有口服活性的，可透過血腦屏障的選擇性 H3 受體拮抗劑，抑制 [3H] 組胺釋放的 Ki 為 4.3 nM。Thioperamide 抑制 [3H] 組胺合成的 Ki 為 31 nM 。靶點(diǎn)
|
H 3 Receptor
|
體外研究
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. |
體內(nèi)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. |