Kretzschmar R, Lehmann H D, Gries J, Kuhne J, Neumann W
Arzneimittelforschung. 1980;30(10):1746-60.
In animal experiments the new imidazoline derivative N-(2-imidazolin-2-yl)-N-(4-indanyl)amine (indanazoline, E-VA-16, as monohydrochloride active substance of Farial) is characterized by a pronounced vasoconstrictive action after local or intravenous application. This is due to a direct action of the compound on alpha-adrenergic receptors. When applied systemically E-VA-16 being a peripherally acting alpha-sympathomimetic induces a rise in blood pressure and a reduction of heart rate and exerts antiphlogistic, spasmolytic, hyperglycemic and diuretic actions. When given by the intranasal route the substance influences blood pressure and heart rate only at concentrations considerably higher than those intended for use in therapy. After enteral administration the effective doses also markedly exceed the single therapeutic doses. There was no evidence of side-effects restricting the use of the drug as compared to other imidazoline derivatives. Studies on the isolated perfused rabbit ear, however, indicated a broader therapeutic range in local application.
在动物实验中,新型咪唑啉衍生物N-(2-咪唑啉-2-基)-N-(4-茚满基)胺(茚达唑啉,E-VA-16,作为Farial的盐酸盐活性物质)在局部或静脉给药后具有明显的血管收缩作用。这是由于该化合物对α-肾上腺素能受体的直接作用。当全身应用时,作为外周作用的α-拟交感神经药的E-VA-16会导致血压升高、心率降低,并具有抗炎、解痉、升高血糖和利尿作用。当通过鼻内途径给药时,该物质仅在浓度远高于治疗预期浓度时才会影响血压和心率。经肠给药后,有效剂量也明显超过单次治疗剂量。与其他咪唑啉衍生物相比,没有证据表明存在限制该药物使用的副作用。然而,对离体灌注兔耳的研究表明,局部应用时具有更宽的治疗范围。