- 英文名称
- GTS-21 dihydrochloride
- 分子式
- C19H22Cl2N2O2
- 分子量
- 381.3
- 中文别名
- (3E)-3-[(2,4-二甲氧基苯基)亚甲基]-3,4,5,6-四氢-2,3'-联吡啶二盐酸盐; GTS-21二盐酸盐; (E)-3-(2,4-二甲氧基苯基)亚甲基)-3,4,5,6-四氢-2,3'-联吡啶二盐酸盐; (E)-3-(2,4-二甲氧基苄亚基)-3,4,5,6-四氢-2,3'-联吡啶 盐酸盐; (1:2),(3E)-3-[(2,4-二甲氧基苯基)亚甲基]-3,4,5,6-四氢-2,3-联吡啶盐酸盐; 3-(2,4-dimethoxybenzylidene)anabaseine; 3-[(3E)-3-[(2,4-dimethoxyphenyl)methylidene]-5,6-dihydro-4H-pyridin-2-yl]pyridine dihydrochloride; 3-(2,4-Dimethoxy-benzyl)-3,4,5,6-tetrahydro-[2,3']bipyridinyl; 3-(2,4)-DiMethoxybenzylidineanabaseine; GTS-21 (DMXB-A); 3-(2,4-DiMethoxy-benzyl)-3,4,5,6-tetrahydro-[2,3']bipyridinyl Dihydrochloride; (3E)-3-[(2,4-Dimethoxyphenyl)methylene]-3,4,5,6-tetrahydro-2,3'-Bipyridine dihydrochloride; DMBX-anabaseine; 3-(2,4-Dimethoxybenzyl)-3,4,5,6-tetrahydro-2,3'-bipyridine; (3E)-3-(2,4-Dimethoxybenzylidene)-3,4,5,6-tetrahydro-2,3'-bipyridine; GTS-21; DMXB-A; GTS 21 2HCl; GTS-21 (dihydrochloride)
- 用途
- 化学合成;作为选择性α7烟碱乙酰胆碱受体(α7-nAChR)激动剂,具有抗炎和增强认知活性;是α4β2(human α4β2: Ki=20 nM)和5-HT3A受体(IC50=3.1 μM)拮抗剂;体外研究显示其对人α4β2 nAChR结合力(Ki=20 nM)比人α7-nAChR强100倍,对人α4β2和α7 nAChR的效力分别比(-)-尼古丁弱18和2倍;体内研究中,C57BL6小鼠经12 Gy辐射诱导肺损伤模型,腹腔注射4 mg/kg GTS-21(连续1、3、7、14、21天)可减少肺炎症浸润和纤维化。