11-((2-((二乙氨基)甲基)-1-哌啶基)乙酰基)-5,11-二氢-(6H)-吡啶并[2.3-B][1.4]苯并二氮杂-6-酮
| 中文名称 | 11-((2-((二乙氨基)甲基)-1-哌啶基)乙酰基)-5,11-二氢-(6H)-吡啶并[2.3-B][1.4]苯并二氮杂-6-酮 |
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| 中文同义词 | 11-((2-((二乙氨基)甲基)-1-哌啶基)乙酰基)-5,11-二氢-(6H)-吡啶并[2.3-B][1.4]苯并二氮杂-6-酮;化合物 T16411;化合物OTENZEPAD;11-(2-(2-((二乙基氨基)甲基)哌啶-1-基)乙酰基)-5H-苯并[E]吡啶并[3,2-B][1,4]二氮杂卓-6(11H)-酮;11-[[2-[(二乙氨基)甲基]-1-哌啶基]乙酰基]-5,11-二氢-6H-吡啶基[2,3-B][1,4]苯二氮卓-6-酮 |
| 英文名称 | 11-[[2-[(DIETHYLAMINO)METHYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE |
| 英文同义词 | 11-[[2-[(DIETHYLAMINO)METHYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE;AF-DX 116;6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one,5,11-dihydro-11-((2-((diethylamino)m;ethyl)-7-piperidinyl)acetyl)-;11-((2-((Diethylamino)methyl)-1-piperidinyl)acetyl)-5,11-dihydro-(6H)-pyrido[2.3-b][1.4]benzodiazepin-6-one;6H-Pyrido(2,3-B)(1,4)benzodiazepin-6-one, 11-((2-((diethylamino)methyl)-1-piperidinyl)acetyl)-5,11-dihydro-;6H-Pyrido(2,3-B)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((2-((diethylamino)methyl)-7-piperidinyl)acetyl)-;Brn 4212983 |
| CAS号 | 102394-31-0 |
| 分子式 | C24H31N5O2 |
| 分子量 | 421.54 |
| EINECS号 | |
| 相关类别 | Acetylcholine receptor;Muscarinic |
| Mol文件 | 102394-31-0.mol |
| 结构式 | ![11-((2-((二乙氨基)甲基)-1-哌啶基)乙酰基)-5,11-二氢-(6H)-吡啶并[2.3-B][1.4]苯并二氮杂-6-酮 结构式](CAS/GIF/102394-31-0.gif) |
11-((2-((二乙氨基)甲基)-1-哌啶基)乙酰基)-5,11-二氢-(6H)-吡啶并[2.3-B][1.4]苯并二氮杂-6-酮 性质
| 沸点 | 573.2±45.0 °C(Predicted) |
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| 密度 | 1.171 |
| 储存条件 | room temp |
| 溶解度 | 在DMSO中的溶解度为5mg/mL（透明溶液；加热） |
| 酸度系数(pKa) | 11.29±0.20(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
Otenzepad (AF-DX 116) 是一种选择性的、竞争性的 M2 毒蕈碱乙酰胆碱受体拮抗剂，对兔外周肺和大鼠心脏的 IC50 值分别为 640 nM 和 386 nM。
640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart).
Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls.
Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls.
Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory.
| Animal Model: | Forty-eight male Long-Evans rats (325-350 g). |
| Dosage: | 0.25, 0.5, 1.0 and 2.0 mg/kg. |
| Administration: | S.C. on the dorsum of the neck once. |
| Result: | Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect. |
| Animal Model: | Adult male Swiss mice (age 60–70 days; weight 25-30 g). |
| Dosage: | 0.3, 1.0, or 3.0 mg/kg. |
| Administration: | IP once. |
| Result: | Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U 15,15 = 49, p < 0.02, compared with saline-saline-injected control group). |