102394-31-0

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

英文名称 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 结构式

基本信息物理化学性质安全数据图谱信息常见问题列表

基本信息

中文别名

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

英文别名

AF-DX 116
Brn 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-

物理化学性质

沸点573.2±45.0 °C(Predicted)

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

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H315-H319-H335

防范说明P233-P260-P261-P264-P271-P280-P302+P352-P304-P304+P340-P305+P351+P338-P312-P321-P332+P313-P337+P313-P340-P362-P403-P403+P233-P405-P501

危险品标志Xn

危险类别码22

WGK Germany3

图谱信息

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(102394-31-0)核磁图(¹HNMR)

常见问题列表

生物活性

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。

靶点

640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart).

体内研究

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).