基于哌仑西平和替仑西平胺类同系物的毒蕈碱受体探针
MUSCARINIC RECEPTOR PROBES BASED ON AMINE CONGENERS OF PIRENZEPINE AND TELENZEPINE.
作者信息
Jacobsont Kenneth A, Kartont Yishai, Baumgold Jesse
机构信息
Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Bethesda, MD 20892.
Department of Radiology, George Washington University, Washington D.C., 20037.
出版信息
Bioorg Med Chem Lett. 1992 Aug;2(8):845-850. doi: 10.1016/s0960-894x(00)80542-9.
The N-methyl groups of pirenzepine and telenzepine (M-antagonists) were modified to produce chemically functionalized N-alkyl analogs using a "functionalized congener" approach. The derivatives were tested in binding assays vs. [H]N-methylscopotamine in rat forebrain and cardiac membranes. The potency/selectivity were highly dependent on substitutions of the N-methyl group. The affinity in a series of -alkyl amino derivatives progressively increased with the number of methylene groups. The amines were acylated with various reporter groups resulting in molecular probes of nanomolar affinity. The effect of chain length on aryl isothiocyanate affinity labels is explored.
通过“功能化同系物”方法对哌仑西平和替仑西平（M拮抗剂）的N-甲基进行修饰，以制备化学功能化的N-烷基类似物。在结合试验中，使用大鼠前脑和心脏膜中的[H]N-甲基东莨菪碱对这些衍生物进行了测试。效力/选择性高度依赖于N-甲基的取代情况。在一系列烷基氨基衍生物中，亲和力随着亚甲基数量的增加而逐渐提高。用各种报告基团对胺进行酰化，得到了具有纳摩尔亲和力的分子探针。研究了链长对芳基异硫氰酸酯亲和标记的影响。
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