Ruffolo R R, Rice P J, Patil P N, Hamada A, Miller D D
Eur J Pharmacol. 1983 Jan 21;86(3-4):471-5. doi: 10.1016/0014-2999(83)90199-1.
The enantiomers of 2-(3,4, alpha-trihydroxybenzyl)imidazoline and the corresponding desoxy derivative, 2-(3,4-dihydroxybenzyl)imidazoline, were evaluated at alpha 1- and alpha 2-adrenergic receptors to test the applicability of the Easson-Stedman hypothesis to the imidazoline class of alpha-adrenergic agonists. A series of closely related phenethylamines was included for comparison. The Easson-Stedman hypothesis states that optically active adrenergic agonists possessing an asymmetric hydroxyl-substituted benzylic carbon atom will have the following relative potencies: R(-) greater than S(+) = desoxy. While the phenethylamines were found to adhere to the Easson-Stedman hypothesis at both alpha 1- and alpha 2-adrenergic receptors, the optically active imidazolines did not. These findings further support our previous observations that the phenethylamines and imidazolines may interact differently with alpha-adrenergic receptors.
对2-(3,4,α-三羟基苄基)咪唑啉及其相应的脱氧衍生物2-(3,4-二羟基苄基)咪唑啉的对映体在α1和α2肾上腺素能受体上进行了评估，以测试伊森-斯蒂德曼假说对咪唑啉类α肾上腺素能激动剂的适用性。还纳入了一系列密切相关的苯乙胺用于比较。伊森-斯蒂德曼假说指出，具有不对称羟基取代苄基碳原子的光学活性肾上腺素能激动剂将具有以下相对效价：R(-)大于S(+) = 脱氧。虽然发现苯乙胺在α1和α2肾上腺素能受体上均符合伊森-斯蒂德曼假说，但光学活性咪唑啉却并非如此。这些发现进一步支持了我们之前的观察结果，即苯乙胺和咪唑啉可能与α肾上腺素能受体有不同的相互作用。
