Devazepide

Modify Date: 2024-01-10 14:54:51

Devazepide Structure
Devazepide structure
Common Name Devazepide
CAS Number 103420-77-5 Molecular Weight 408.45200
Density 1.31g/cm3 Boiling Point 758.6ºC at 760mmHg
Molecular Formula C25H20N4O2 Melting Point N/A
MSDS Chinese USA Flash Point 412.6ºC
Symbol GHS06
GHS06
Signal Word Danger

 Use of Devazepide


Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders[1].

 Names

Name devazepide
Synonym More Synonyms

 Devazepide Biological Activity

Description Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders[1].
Related Catalog
Target

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

References

[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.

 Chemical & Physical Properties

Density 1.31g/cm3
Boiling Point 758.6ºC at 760mmHg
Molecular Formula C25H20N4O2
Molecular Weight 408.45200
Flash Point 412.6ºC
Exact Mass 408.15900
PSA 77.56000
LogP 3.62930
Vapour Pressure 6.56E-23mmHg at 25°C
Index of Refraction 1.696

 Toxicological Information

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

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H300
Precautionary Statements P264-P301 + P310
Hazard Codes T
Safety Phrases 28-36/37-45
RIDADR UN 2811 6.1 / PGI
RTECS NL5994460

 Articles25

More Articles
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...

 Synonyms

N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide
Devazepida
DEVAZEPIDE
Devazepidum
MK-329
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