Lanier S M, Lanier B, Bakthavachalam V, McGrath C R, Neumeyer J L
Department of Pharmacology, Medical University of South Carolina, Charleston 29425, USA.
Ann N Y Acad Sci. 1995 Jul 12;763:106-11. doi: 10.1111/j.1749-6632.1995.tb32395.x.
Various pharmacologically active compounds with an imidazoline or guanidinium moiety are recognized by membrane bound proteins that appear structurally and functionally distinct from known hormone receptors. Such entities are termed imidazoline binding sites, I receptors, or imidazoline/guanidinium receptive sites (IGRS). To facilitate the identification and structural analysis of IGRS, we developed functionalized molecular probes exhibiting high affinity and selectivity for IGRS. The molecular probes are structurally related to cirazoline, and imidazoline that exhibits high affinity for IGRS in both central and peripheral tissues. The parent molecule 2-[3-aminophenoxy]methyl imidazoline (125I-AMIPI), which was used to identify IGRS in brain and peripheral tissues. 125I-AMIPI was converted to the photosensitive arylazide derivative (125I-AMIPI) and used to identify the M(r) of the ligand binding subunit of IGRS in various tissues including brain, pancreas, kidney, and liver. The results of these studies indicate that there are multiple binding proteins for these molecules that differ in their apparent molecular weight, tissue distribution, intratissue location, and ligand recognition properties.
各种带有咪唑啉或胍基部分的药理活性化合物可被膜结合蛋白识别，这些膜结合蛋白在结构和功能上与已知的激素受体不同。这类实体被称为咪唑啉结合位点、I型受体或咪唑啉/胍基受体位点（IGRS）。为便于对IGRS进行鉴定和结构分析，我们开发了对IGRS具有高亲和力和选择性的功能化分子探针。这些分子探针在结构上与西拉唑啉有关，西拉唑啉是一种在中枢和外周组织中对IGRS均具有高亲和力的咪唑啉。母体分子2-[3-氨基苯氧基]甲基咪唑啉（125I-AMIPI），用于鉴定脑和外周组织中的IGRS。125I-AMIPI被转化为光敏芳基叠氮化物衍生物（125I-AMIPI），并用于鉴定包括脑、胰腺、肾脏和肝脏在内的各种组织中IGRS配体结合亚基的分子量。这些研究结果表明，这些分子存在多种结合蛋白，它们在表观分子量、组织分布、组织内定位和配体识别特性方面存在差异。
