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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

用途

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。

名称

[ CAS 号 ]:
102394-31-0

[ 中文名 ]:
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

[ 英文名 ]:
Otenzepad

[中文别名 ]:

[英文别名 ]:

NPEC-caged-dopamine
ethyl)-7-piperidinyl)acetyl)
AF-DX 116

生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

研究领域 >> 代谢疾病

研究领域 >> 神经疾病

[ 靶点 ]

640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart)[1].

[体内研究]

与注射载体的对照组相比,奥替西泮(0.5,1 mg/kg,s.c.,在大鼠体内)显著改善了win-stay的获得[2]。与载体对照组相比,奥替尼泮(2 mg/kg,s.c.,大鼠体内)显著提高了保留率[2]。Otenzepad(0.3、1.0或3.0 mg/kg,ip,小鼠体内)增强葡萄糖的作用,逆转胰岛素对记忆的影响[3]。动物模型：48只雄性Long-Evans大鼠(325-350g)[2]。用量：0.25、0.5、1.0、2.0mg/kg。给药：颈背部皮下注射一次。结果：0.5mg/kg和1.0mg/kg剂量组较对照组有显著性提高,0.25和2.0mg/kg剂量组无明显影响。动物模型：成年雄性瑞士小鼠(年龄60-70天；体重25-30克)[3]。剂量：0.3、1.0或3.0 mg/kg。管理：IP一次。结果：与生理盐水注射对照组相比,在1.0mg/kg时,尿潴留呈倒U型剂量反应增强(U15,15=49,p<0.02)。

[参考文献]

[1]. Bloom JW, et al. Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116. Life Sci. 1987 Jul 27;41(4):491-6.

[2]. Packard MG, et al. Post-training injection of the acetylcholine M2 receptor antagonist AF-DX 116 improves memory. Brain Res. 1990 Jul 30;524(1):72-6.

[3]. Kopf SR, et al. AF-DX 116, a presynaptic muscarinic receptor antagonist, potentiates the effects of glucose and reverses the effects of insulin on memory. Neurobiol Learn Mem. 1998 Nov;70(3):305-13.

物理化学性质

[ 密度 ]:
1.171 g/cm3

[ 沸点 ]:
573.2ºC at 760 mmHg

[ 分子式 ]:
C₂₄H₃₁N₅O₂

[ 分子量 ]:
421.53500

[ 闪点 ]:
300.5ºC

[ 精确质量 ]:
421.24800

[ PSA ]:
74.23000

[ LogP ]:
3.21440

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV0697000

CHEMICAL NAME :: 6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((2-((diethylamino) methyl)-7-piperidinyl)acetyl)-

CAS REGISTRY NUMBER :: 102394-31-0

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C24-H31-N5-O2

MOLECULAR WEIGHT :: 421.60

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1533 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 83 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

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