Hoefke W, Gaida W, Stähle H
Arzneimittelforschung. 1985;35(1A):424-7.
In anaesthetized rabbits the hypotensive activity of a group of 2,3-disubstituted 2-aryl-imino-imidazolidines was estimated. Compounds with 3-bromo substituents at the phenyl moiety of the molecule are more than or as active as clonidine. Correlations between blood pressure lowering effect and lipophilicity, maximum alpha-adrenergic effects (alpha E') and -log ED50 (pD2') of blood pressure increase in spinalized rats and pKA were calculated. The results show a positive linear correlation between as well partition coefficient as alpha E' and hypotension. The relationship between pD2' and hypotensive. effect is less prominent. pKA seems to have no influence on the blood pressure effects of these compounds.
在麻醉兔身上评估了一组2,3-二取代的2-芳基亚氨基咪唑烷的降压活性。分子中苯基部分带有3-溴取代基的化合物比可乐定更具活性或与之活性相当。计算了降压效果与亲脂性、脊髓麻醉大鼠血压升高的最大α-肾上腺素能效应（αE'）和-log ED50（pD2'）以及pKA之间的相关性。结果表明，分配系数和αE'与低血压之间呈正线性相关。pD2'与降压效果之间的关系不太显著。pKA似乎对这些化合物的血压效应没有影响。
