Thioperamide maleate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Thioperamidemaleate 是一种有效的选择性 H3 受体拮抗剂 (Ki = 4.3 nM)，可抑制 [3H]组胺合成 (Ki = 31 nM)。

Thioperamide maleate is an effective and selective antagonist of H3 receptor (Ki = 4.3 nM) for inhibition of [3H]histamine synthesis (Ki = 31 nM).(In Vitro):Thioperamide maleate (0.01, 0.1, 1, 10, 100 μM) promotes the viability of NE-4C stem cells in a concentration-dependent manner. Thioperamide maleate displays similar potencies at human H4 and H3 receptors with Kis of 43 and 60 nM, respectively. Thioperamide maleate inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide maleate competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM.(In Vivo):In C57BL/6J mice, Thioperamide (5-20 mg/kg; i.p.) facilitates reconsolidation of a contextually-conditioned fear memory.

Thioperamide inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM.Thioperamide (0.01-100 μM; 24 hours) promotes the viability of NE-4C stem cells in a concentration-dependent manner.Thioperamide displays similar potencies at human H4 and H3 receptors (Ki=43 and 60 nM, respectively).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.

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.

MR-12842 maleate

GPCR/G Protein

Histamine Receptor

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148440-81-7

408.52

C19H28N4O4S

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL

OC(=O)\C=C/C(O)=O.S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1

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(-20℃)

With Ice Pack

≥ 2 years