地伐西匹

地伐西匹用途

Devazepide (L-364,718) 是一种有效、竞争性、选择性、可口服的非肽类胆囊收缩素受体 (cholecystokinin (CCK) receptor) 拮抗剂,对大鼠胰腺、牛胆囊和豚鼠大脑 CCK 受体的 IC50 值分别为 81 pM,45 pM 和 245 nM。Devazepide (L-364,718) 对肠胃疾病有效。

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地伐西匹名称

[ CAS 号 ]:
103420-77-5

[ 中文名 ]:
地伐西匹

[ 英文名 ]:
Devazepide

[英文别名 ]:

Devazepida
DEVAZEPIDE
Devazepidum
MK-329

地伐西匹生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 内分泌

研究领域 >> 其他

[ 靶点 ]

IC50: 45 pM (Rat pancreatic CCK receptor), 81 pM (Bovine gallbladder CCK receptor), 245 nM (Guinea pig brain CCK receptor)[1]

[参考文献]

[1]. Chang RS, et al. Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist. Proc Natl Acad Sci U S A. 1986 Jul;83(13):4923-6.

地伐西匹物理化学性质

[ 密度 ]:
1.31g/cm3

[ 沸点 ]:
758.6ºC at 760mmHg

[ 分子式 ]:
C₂₅H₂₀N₄O₂

[ 分子量 ]:
408.45200

[ 闪点 ]:
412.6ºC

[ 精确质量 ]:
408.15900

[ PSA ]:
77.56000

[ LogP ]:
3.62930

[ 外观性状 ]:
白色至类白色粉末

[ 蒸汽压 ]:
6.56E-23mmHg at 25°C

[ 折射率 ]:
1.696

[ 储存条件 ]:
库房通风低温干燥,与氧化剂、碱类、食品添加剂分开存放

地伐西匹MSDS

详细MSDS(安全技术说明书)

地伐西匹毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NL5994460

CHEMICAL NAME :: 1H-Indole-2-carboxamide, N-(2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodi azepin-3-yl)-, (S)-

CAS REGISTRY NUMBER :: 103420-77-5

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C25-H20-N4-O2

MOLECULAR WEIGHT :: 408.49

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 14,862,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 14,862,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 1 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 14,862,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 1 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 14,862,1989

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地伐西匹安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
P264-P301 + P310

[ 危害码 (欧洲) ]:
T

[ 安全声明 (欧洲) ]:
28-36/37-45

[ 危险品运输编码 ]:
UN 2811 6.1 / PGI

[ RTECS号 ]:
NL5994460

地伐西匹文献

Ongoing ingestive behavior is rapidly suppressed by a preabsorptive, intestinal "bitter taste" cue.

Am. J. Physiol. Regul. Integr. Comp. Physiol. 301(5) , R1557-68, (2011)

The discovery that cells in the gastrointestinal (GI) tract express the same molecular receptors and intracellular signaling components known to be involved in taste has generated great interest in po...

Behavioral and cortical EEG evaluations confirm the roles of both CCKA and CCKB receptors in mouse CCK-induced anxiety.

Behav. Brain Res. 237 , 325-32, (2013)

This study investigated the roles of cholecystokinin (CCK)(A) and CCK(B) receptors on CCK-4-induced anxiety-like behaviors in mice through behavioral and neural evaluations. Anxiety-like behaviors in ...

Synergistic effect of CART (cocaine- and amphetamine-regulated transcript) peptide and cholecystokinin on food intake regulation in lean mice.

BMC Neurosci. 9 , 101, (2008)

CART (cocaine- and amphetamine-regulated transcript) peptide and cholecystokinin (CCK) are neuromodulators involved in feeding behavior. This study is based on previously found synergistic effect of l...

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