Meclizine (Meclozine) dihydrochloride 是一种抗组胺剂 (antihistamine)，可逆地抑制组胺与 H1 受体的相互作用。Meclizine dihydrochloride 是哌嗪类 H1 拮抗剂。Meclizine dihydrochloride 是一种有效的抗晕车剂。Meclizine dihydrochloride 可透过血脑屏障，可用于多聚谷氨酰胺毒性障碍（例如亨廷顿舞蹈症）方面的研究。Meclizine dihydrochloride 是小鼠组成型雄甾烷受体 (CAR) 激动剂，是人 CAR 的反向激动剂。
| CAS No. | 1104-22-9 |
| 生物活性 | Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. |
| 分子式 | C25H27N2Cl.2[HCl] |
| 分子量 | 463.87 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 92 mg/mL (198.33 mM; Need ultrasonic) |
| 体内研究 | Meclizine (Meclozine; 10-100 mg/kg; ip) dihydrochloride protects mouse against kidney ischemia. Pretreatment with 100 mg/kg of Meclizine, 17 or 24 h prior to ischemia shows kidney protection in mice. Meclizine dihydrochloride reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis. |
| 体外研究 | Meclizine (Meclozine; 50 µM; 24 hours) dihydrochloride significantly increases cell survival in STHdh cells at 24 h after the removal of serum, evidently by suppressing apoptosis, based on caspase 3 and 7 cleavage. The rescue is dose-dependent with an EC50 of 17.3 µm, and a maximum efficacy of 218% increased survival over vehicle. Meclizine dihydrochloride protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdh) and wild-type (STHdh) striatal cells. |
| 纯度及产品资料 | 98% |
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