Devazepide
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.
All Tocris products are intended for laboratory research use only.
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 solvent 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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References
References are publications that support the products' biological activity.
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) Metformin 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, supplier, Selective, orally, active, CCK1, receptor, antagonists, Cholecystokinin1, Receptors, L364718, MK329, L-364,718, MK, 329, CCK1, Receptor, CCK1, Receptor, Tocris Bioscience
7 Citations for Devazepide
Citations are publications that use Tocris products. Selected citations for Devazepide include:
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 morphine dependence. Front Mol Neurosci 13 63 PMID: 22682150
D'Agostino et al (2016) Appetite controlled by a cholecystokinin nucleus of the solitary tract to hypothalamus neurocircuit. BMC Neurosci 5 PMID: 26974347
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
Cheung et al (2009) Intestinal cholecystokinin controls glucose production through a neuronal network. Cell Metab 10 99 PMID: 19656488
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
Do you know of a great paper that uses Devazepide from Tocris? If so please let us know.
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