ALVAMELINE
|
|
- CAS号:
- 120241-31-8
- 英文名:
- ALVAMELINE
- 英文别名:
- Lu 25-109;ALVAMELINE;3-(2-Ethyl-2H-tetrazol-5-yl)-1,2,5,6-tetrahydro-1-methylpyridine;Pyridine, 3-(2-ethyl-2H-tetrazol-5-yl)-1,2,5,6-tetrahydro-1-methyl-;2-Ethyl-5-(1-methyl-1,2,5,6-tetrahydro-3-pyridyl)-2H-tetrazole tartrate;5-(2-Ethyl-2H-tetrazol-5-yl)-1,2,3,6-tetrahydro-1-methylpyridine tartrate;3-(2-Ethyl-2H-tetrazol-5-yl)-1,2,5,6-tetrahydro-1-methyl-pyridine tartrate
- 中文名:
- ALVAMELINE
- 中文别名:
- 阿伐美林;化合物 T14197
- CBNumber:
- CB92451399
- 分子式:
- C9H15N5
- 分子量:
- 193.25
- MOL File:
- 120241-31-8.mol
|
|
|
ALVAMELINE化学性质
-
沸点:
-
342.1±52.0 °C(Predicted)
-
|
-
密度:
-
1.25±0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
2-8°C
-
|
-
溶解度:
-
Soluble in DMSO
-
|
-
酸度系数(pKa):
-
7.29±0.40(Predicted)
-
|
ALVAMELINE性质、用途与生产工艺
Alvameline (Lu25-109)是M1的部分激动剂,也是M2/M3拮抗剂。
Alvameline is metabolized by human liver microsomes to Lu 31-126 mainly by CYP2D6; to Lu 29-297 and Lu 25-077 mainly by CYP1A2, CYP2A6, CYP2C19, and CYP3A4; and to Lu 32-181 by CYP1A2 and possibly by CYP2C19. One metabolite, Lu 32-181, could be reduced back to alvameline, a reaction not inhibited by the applied cytochrome P-450 inhibitors.
Alvameline competitively and effectively antagonizes carbachol-induced contractions and contractions induced by electrical field stimulation in human detrusor muscle. Alvameline produces a concentration-dependent rightward shift of the concentration-response curves for carbachol in both human and pig detrusor, the pK
b
values being 6.2 and 5.8. Contractions induced by electrical field stimulation in human detrusor are almost completely inhibited by 100 μM alvameline. In contrast, electrical field stimulation-induced contractions in pig detrusor are less sensitive to alvameline, resulting in a final inhibition of 32% with the highest concentration used (100 μM). Alvameline has been shown to improve cognitive
function following traumatic brain injury in rats. Alvameline treated rats causes a 13% and 5% decrease in the medial septal nucleus, a 48 and 23% decrease in the vertical limb nucleus of the diagonal band, and a 51 and 28% decrease in the nucleus basalis magnocellularis, respectively.
ALVAMELINE
上下游产品信息
上游原料
下游产品
120241-31-8, ALVAMELINE 相关搜索:
- 化合物 T14197
- 阿伐美林
- 120241-31-8
- Pyridine, 3-(2-ethyl-2H-tetrazol-5-yl)-1,2,5,6-tetrahydro-1-methyl-
- 5-(2-Ethyl-2H-tetrazol-5-yl)-1,2,3,6-tetrahydro-1-methylpyridine tartrate
- 3-(2-Ethyl-2H-tetrazol-5-yl)-1,2,5,6-tetrahydro-1-methyl-pyridine tartrate
- 2-Ethyl-5-(1-methyl-1,2,5,6-tetrahydro-3-pyridyl)-2H-tetrazole tartrate
- Lu 25-109
- 3-(2-Ethyl-2H-tetrazol-5-yl)-1,2,5,6-tetrahydro-1-methylpyridine
- ALVAMELINE