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编 号:F453914
分子式:C21H26BrNO3
分子量:420.34
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10mM*1mL in DMSO
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100mg
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500mg
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生物活性:
Mepenzolate bromide is an orally administered muscarinic receptor antagonist with Kis of 0.68 and 2.6 nM for hM2R and hM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome.Mepenzolate bromide is a GPR109A inhibitor.

体内研究:
Mepenzolate bromide 是一种 GPR109A 受体阻断剂,可消除烟酸对体重、结肠湿重以及结肠髓过氧化物酶 (MPO) 和 VEGF 水平的有益影响。 Mepenzolate bromide 是一种毒蕈碱拮抗剂。气管内给药或吸入 Mepenzolate bromide 可降低弹性蛋白酶诱导的空腔扩大和呼吸功能障碍的严重程度。由于其抗炎和支气管扩张活性,甲哌佐酯溴可能是处理慢性阻塞性肺疾病 (COPD) 的有效药物。Animal Model:Adult male Wistar rats, weighing 150-200?g
Dosage:5 ?mg/kg
Administration:Intraperitoneal injection
Result:Abolished the protective effect of niacin against iodoacetamide-induced rise in colon wet weight as well as the colonic levels of both MPO and VEGF.
Animal Model:ICR mice (4-6 weeks old, male) and DBA/2 mice (5 weeks old, female)
Dosage:0.04, 0.38, 3.8, 38 μg/kg; 45.2 and 226 μg per chamber
Administration:"0.04, 0.38, 3.8, 38 μg/kg administered intratracheally once daily for 14 days 45.2 and 226 μg per chamber by inhalation once daily for 14 days"
Result:The simultaneous daily intratracheal administration suppressed this enlargement in a dose-dependent manner.The inhalation route?was similar to those observed with the intratracheal mode of administration.

体外研究:
Mepenzolate 不仅通过毒蕈碱受体非依赖性机制发挥抗炎作用,而且通过毒蕈碱受体依赖性机制发挥支气管扩张作用。Mepenzolate 是一种亚型非特异性毒蕈碱拮抗剂,其支气管扩张作用和对肠蠕动的抑制作用可通过其对 M3R 的拮抗作用来解释。
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