102394-31-0
中文名稱
11-((2-((二乙氨基)甲基)-1-哌啶基)乙酰基)-5,11-二氫-(6H)-吡啶并[2.3-B][1.4]苯并二氮雜-6-酮
英文名稱
11-[[2-[(DIETHYLAMINO)METHYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE
CAS
102394-31-0
分子式
C24H31N5O2
分子量
421.54
MOL 文件
102394-31-0.mol
更新日期
2023/11/10 17:23:55
102394-31-0 結(jié)構(gòu)式
基本信息
中文別名
11-((2-((二乙氨基)甲基)-1-哌啶基)乙?；?-5,11-二氫-(6H)-吡啶并[2.3-B][1.4]苯并二氮雜-6-酮 英文別名
AF-DX 116Brn 4212983
(100158-38-1) otenzepad
ethyl)-7-piperidinyl)acetyl)-
6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one,5,11-dihydro-11-((2-((diethylamino)m
11-(2-(2-((Diethylamino)methyl)piperidin-1-yl)acetyl)-5H-benzo[e]pyrido[3,2-b][1,4]diazepin-6(11H)-one
11-[[2-[(DIETHYLAMINO)METHYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE
11-[2-[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, 5,11-dihydro-11-((2-((diethylamino)methyl)-7-piperidinyl)acetyl)-
6H-Pyrido(2,3-B)(1,4)benzodiazepin-6-one, 11-((2-((diethylamino)methyl)-1-piperidinyl)acetyl)-5,11-dihydro-
物理化學(xué)性質(zhì)
沸點(diǎn)573.2±45.0 °C(Predicted)
密度1.171
儲存條件room temp
溶解度在DMSO中的溶解度為5mg/mL（透明溶液；加熱）
酸度系數(shù)(pKa)11.29±0.20(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
Otenzepad (AF-DX 116) 是一種選擇性的、競爭性的 M2 毒蕈堿乙酰膽堿受體拮抗劑，對兔外周肺和大鼠心臟的 IC50 值分別為 640 nM 和 386 nM。靶點(diǎn)
640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart).
體內(nèi)研究
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). |