Devazepide

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Cat.No. 2304 - Devazepide | C25H20N4O2 | CAS No. 103420-77-5
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)
Datasheet
Citations (4)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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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

4 Citations for Devazepide

Citations are publications that use Tocris products. Selected citations for Devazepide include:

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

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

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


Do you know of a great paper that uses Devazepide from Tocris? If so please let us know.

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Literature in this Area

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Peptides Involved in Appetite Modulation

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Pathways for Devazepide

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