233275-76-8
中文名称
MK 0343
CAS
233275-76-8
分子式
C19H17F2N7O
分子量
397.38
MOL 文件
233275-76-8.mol
更新日期
2023/03/20 15:41:21
233275-76-8 结构式
基本信息
中文别名
7-环丁基-3-(2,6-二氟苯基)-6-((1-甲基-1H-1,2,4-三氮唑-5-乙基)甲氧基)-[1,2,4]三氮唑[4,3-B]哒嗪 英文别名
MK 0343MRK-409
MK-0343 >=98% (HPLC)
7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazo[4,3-b]pyridazine
7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-b]pyridazine
1,2,4-Triazolo[4,3-b]pyridazine, 7-cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-Methyl-1H-1,2,4-triazol-5-yl)Methoxy]-
物理化学性质
密度1.57±0.1 g/cm3(Predicted)
储存条件Inert atmosphere,2-8°C
溶解度DMSO：可溶10mg/mL，澄清
酸度系数(pKa)2.11±0.10(Predicted)
形态粉末
颜色白色至米色
常见问题列表
生物活性
MK0343 (MRK-409) 是一种口服生物可利用的 GABAA 受体亚型选择性部分激动剂。MK0343 是一种非镇静的抗焦虑药物。靶点
Ki: 0.22 nM (rGABA A α1), 0.4 nM (rGABA A α2) , 0.21 nM (rGABA A α3), 78 nM (rGABA A α4), 0.23 nM (rGABA A α5), 980 nM (rGABA A α6)
体内研究
MK0343 readily penetrates the brain in rats and occupies the benzodiazepine site of GABAA receptors, measured using an in vivo [
3
H]flumazenil binding assay, with an Occ
50
of 2.2 mg/kg p.o. and a corresponding plasma EC
50
of 115 ng/mL.
| Animal Model: | Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics) |
| Dosage: | 1, 2 or 3 mg/kg |
| Administration: | Oral administration |
| Result: | Readily penetrated the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ 50 of 2.2 mg/kg p.o. and a corresponding plasma EC 50 of 115 ng/mL. |