BETA-CARBOLINES AS BENZODIAZEPINE RECEPTOR LIGANDS .2. SYNTHESIS AND BENZODIAZEPINE RECEPTOR AFFINITY OF BETA-CARBOLINE-3-CARBOXYLIC ACID-AMIDES
BETA-CARBOLINES AS BENZODIAZEPINE RECEPTOR LIGANDS .2. SYNTHESIS AND BENZODIAZEPINE RECEPTOR AFFINITY OF BETA-CARBOLINE-3-CARBOXYLIC ACID-AMIDES
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DOI：
10.1002/jps.2600740620
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发表时间：
1985-01-01
影响因子：
3.8
通讯作者：
SCHUNACK, WG
中科院分区：
文献类型：
--
作者：
LIPPKE, KP;MULLER, WE;SCHUNACK, WG
众多的β-咔啉-3-甲酰胺是通过β-甲酰胺化反应合成的。咔啉-3-羧酸，其中各种氨基酸和氨基酸酯用作胺组分，并测试它们对小鼠脑膜中苯并二氮杂受体的亲和力。标题化合物在低微摩尔范围内具有亲和力。讨论了结果与可能的β-含有苯二氮卓受体内源性配体的咔啉结构。
Numerous .beta.-carboline-3-carboxamides were synthesized by amidation of .beta.-carboline-3-carboxylic acid, with various amino acids and amino acid esters serving as amine components, and tested with respect to their affinity for the benzodiazepine receptor in mouse brain membranes. The title compounds have affinities in the low micromolar range. The results are discussed with respect to their relevance for a possible .beta.-carboline structure containing the endogenous ligand of the benzodiazepine receptor.