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Submit ReviewDevazepide
Description: Selective, orally active CCK1 receptor antagonist
Alternative Names: L-364,718, MK 329
Chemical Name: N-[(3S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide
Purity: ≥99% (HPLC)
Biological Activity
Potent, orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. Blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.
Technical Data
| M. Wt | 408.46 |
| Formula | C25H20N4O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 103420-77-5 |
| PubChem ID | 443375 |
| InChI Key | NFHRQQKPEBFUJK-HSZRJFAPSA-N |
| Smiles | CN1C2=CC=CC=C2C(=N[C@H](NC(=O)C2=CC3=C(N2)C=CC=C3)C1=O)C1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.85 | 100 | |
| ethanol | 20.42 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 408.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.45 mL | 12.24 mL | 24.48 mL |
| 5 mM | 0.49 mL | 2.45 mL | 4.9 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.45 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Ebenezer (2002) Effects of intracerebroventricular administration of the CCK1 receptor antagonist devazepide on food intake in rats. Eur.J.Pharmacol. 441 79 PMID: 12007923
Reidelberger et al (2003) Effects of peripheral CCK receptor blockade on food intake in rats. Am.J.Physiol.Reg.Integr.Comp.Physiol. 285 R429 PMID: 12738611
Ritter (2004) Increased food intake and CCK receptor antagonists: beyond abdominal vagal afferents. Am.J.Physiol.Reg.Integr.Comp.Physiol. 286 R991 PMID: 15142854
Duca et al (2015) MetF. activates a duodenal Ampk-dependent pathway to lower hepatic glucose production in rats. Nat.Med. 21 506 PMID: 25849133
If you know of a relevant reference for Devazepide, please let us know.
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Keywords: Devazepide, Devazepide supplier, Selective, orally, active, CCK1, receptor, antagonists, Cholecystokinin1, Receptors, L364718, MK329, L-364,718, MK, 329, Receptor, 2304, Tocris Bioscience
9 Citations for Devazepide
Citations are publications that use Tocris products. Selected citations for Devazepide include:
Cheung et al (2009) Intestinal cholecystokinin controls glucose production through a neuronal network. Cell Metab 10 99 PMID: 19656488
Argueta et al (2019) Cannabinoid CB1 Receptors Inhibit Gut-Brain Satiation Signaling in Diet-Induced Obesity. Front Physiol 10 704 PMID: 31281260
Blevins et al (2012) Alterations in activity and energy expenditure contribute to lean phenotype in Fischer 344 rats lacking the cholecystokinin-1 receptor gene. Am J Physiol Regul Integr Comp Physiol 303 R1231 PMID: 23115121
Schier et al (2011) Ongoing ingestive behavior is rapidly suppressed by a preabsorptive, intestinal "bitter taste" cue. Am J Physiol Regul Integr Comp Physiol 301 R1557 PMID: 21865540
Blouet and Schwartz (2012) Duodenal lipid sensing activates vagal afferents to regulate non-shivering brown fat thermogenesis in rats. PLoS One 7 e51898 PMID: 23251649
D'Agostino et al (2016) Appetite controlled by a cholecystokinin nucleus of the solitary tract to hypothalamus neurocircuit. BMC Neurosci 5 PMID: 26974347
Saia et al (2014) Cholecystokinin inhibits inducible nitric oxide synthase expression by lipopolysaccharide-stimulated peritoneal macrophages. Mediators Inflamm 2014 896029 PMID: 25125801
Wen et al (2012) Cholecystokinin receptor-1 mediates the inhibitory effects of exogenous cholecystokinin octapeptide on cellular mor. dependence. Front Mol Neurosci 13 63 PMID: 22682150
Bauer et al (2018) Lactobacillus gasseri in the Upper Small Intestine Impacts an ACSL3-Dependent Fatty Acid-Sensing Pathway Regulating Whole-Body Glucose Homeostasis. Cell Metab 27 572 PMID: 29514066
Do you know of a great paper that uses Devazepide from Tocris? Please let us know.
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