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Steryl beta-D-glucoside medicaments - with haemostatic, vascular-strengthening and anti-shock activity

机译:硬脂基β-D-葡萄糖苷药物-具有止血,增强血管和抗休克活性

摘要

Medicaments with haemostatic, vascular-strengthening and anti-shock activity contain one or more stearyl beta-D-glucosides of formula (I): (where R1 is beta-sitosteryl, campesteryl, stigmasterol or cholesteryl; R2 is H or palmitoyl). Cpds. (I) have low toxicity (LD50 300 mg/kg, p.o., mouse) and, compared with carbazochrome sodium sulphonate, have 12-22 times its haemostatic activity against amputation-induced haemorrhage nED50 = 1.66-2.88 mg/kg, p.o., mouse), 7-9.5 times its vascular-strengthening activity against vacuum-incuded pulmonary haemorrhage (ED50 = 42.2-58.0 mg/kg, p.o., mouse), 100 times its activity against histamine-, lecithinase- and formalin-induced increases in vascular permeability, and 3 times its activity against passive systemic anaphylaxis.
机译:具有止血,增强血管和抗休克活性的药物包含一种或多种式(I)的硬脂基β-D-葡糖苷:(其中R1为β-谷甾醇基,菜油甾醇基,豆甾醇或胆固醇基; R2为H或棕榈酰基)。 Cpds。 (I)具有低毒性(LD50> 300 mg / kg,口服,小鼠),并且与咔唑铬磺酸钠相比,其抗截肢出血的止血活性为nED50 = 1.66-2.88 mg / kg,口服,小鼠)的抗血管性肺出血(ED50 = 42.2-58.0 mg / kg,po,小鼠)的血管增强活性的7-9.5倍,抗组胺,卵磷脂酶和福尔马林诱导的血管增加活性的100倍渗透性,是抗被动系统过敏反应活性的3倍以上。

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