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Submit ReviewDevazepide
说明： Selective, orally active CCK1 receptor antagonist
别名： L-364,718,MK 329
化学名： N-[(3S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide
纯度： ≥99% (HPLC)
生物活性 for Devazepide
Devazepide is a 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.
技术数据 for Devazepide
| 分子量 | 408.46 |
| 公式 | C25H20N4O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Devazepide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 40.85 | 100 | |
| ethanol | 20.42 | 50 |
制备储备液 for Devazepide
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Devazepide
参考文献 for Devazepide
参考文献是支持产品生物活性的出版物。
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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关键词: Devazepide, Devazepide supplier, Selective, orally, active, CCK1, receptor, antagonists, Cholecystokinin1, Receptors, L364718, MK329, L-364,718, MK, 329, Receptor, 2304, Tocris Bioscience
9 篇 Devazepide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Devazepide 的部分引用包括：
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
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
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
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
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
Argueta et al (2019) Cannabinoid CB1 Receptors Inhibit Gut-Brain Satiation Signaling in Diet-Induced Obesity. Front Physiol 10 704 PMID: 31281260
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
Cheung et al (2009) Intestinal cholecystokinin controls glucose production through a neuronal network. Cell Metab 10 99 PMID: 19656488
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Devazepide 的评论
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Works for block CCKA receptor..
By
Donovan Argueta on 02/10/2021
分析类型： In Vivo
种属： Mouse
细胞系/组织： CCK-eGFP-positive cells
We used low-fat chow fed mice and that is blocked by co-administration with the CCKA receptor antagonist by devazepide treatment.0.1 mg per kg for devazepide treatment
Devazepide was dissolved in vehicle consisting of 7.5% DMSO, 7.5% Tween80, and 85% sterile saline, and warmed in a water bath to ensure solubility.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.