咪唑啉类化合物的甲基化导致 α₂-肾上腺素能受体亲和力丧失。选择性 I₁ 咪唑啉受体配体的合成与生物评价。
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.
机构信息
Laboratoire de Neurobiologie et Pharmacologie Cardiovasculaire, EA 4438, Université de Strasbourg, Faculté de Médecine, 11, rue Humann, F-67000 Strasbourg, France.
出版信息
Bioorg Med Chem. 2012 Aug 1;20(15):4710-5. doi: 10.1016/j.bmc.2012.06.008. Epub 2012 Jun 9.
Methylated analogues of imidazoline related compounds (IRC) were prepared; their abilities to bind I(1) imidazoline receptors (I(1)Rs), I(2) imidazoline binding sites (I(2)BS) and α(2)-adrenoceptor subtypes (α(2)ARs) were assessed. Methylation of the heterocyclic moiety of IRC resulted in a significant loss of α(2)AR affinity. Amongst the selective ligands obtained, LNP 630 (4) constitutes the first highly selective I(1)R agent showing hypotensive activity after intravenous administration.
合成了咪唑啉相关化合物（IRC）的甲基化类似物；评估了它们与 I(1)咪唑啉受体（I(1)Rs）、I(2)咪唑啉结合位点（I(2)BS）和 α(2)-肾上腺素能受体亚型（α(2)ARs）结合的能力。IRC 杂环部分的甲基化导致与 α(2)AR 的亲和力显著降低。在所获得的选择性配体中，LNP 630（4）是第一个具有降压活性的高度选择性 I(1)R 配体，静脉给药后具有降压活性。
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