- SR 27897
- CCK Octapeptide, non-sulfated
- Proglumide sodium salt
- A-71623
| DevazepideCCK1 (CCK-A) receptor antagonist, orally active |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 103420-77-5 | SDF | Download SDF |
| Chemical Name | (S)-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-1H-indole-2-carboxamide | ||
| Canonical SMILES | O=C1N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N[C@@H]1NC(C4=CC5=CC=CC=C5N4)=O | ||
| Formula | C25H20N4O2 | M.Wt | 408.46 |
| Solubility | <40.85mg l="" in="" dmso;=""><20.42mg l="" in="" ethanol=""> | Storage | Store at -20°C |
| Physical Appearance | White solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Devazepide is a potent CCK-A receptor antagonist with IC50 of 0.26 nM. [1]
Cholecystokinin (CCK) has long been recognized as the dominant regulator of gallbladder contraction. The cholecystokinetic activity of different fragments of CCK in human has been established in several studies both in vivo and in vitro. There are two subtypes of CCK receptor that were identified, CCK-A and CCK-B. CCK-A are mainly located in peripheral tissues but also found in brain, while CCK-B distribute throughout the rodent central nervous system.
Devazeptide inhibitory effect against sulphated C-terminal octapeptide of cholecystokinin (CCK-8) on total [3H] inositol phosphate accumulation in CHO-AI cells was investigated. The results revealed that devazepide possesses an inhibitory effect with IC50 of 0.26 ± 0.06 nM. CCK-8 is considered to be the most potent endogenous anti-opiate agent. Morphine analgesia could be antagonized by treatment of CCK-8. However, the effect of CCK-8 could be reversed by devazeptide which could also potentiate analgesia of morphine greatly at doses of 50ng and 200ng. [2, 3]
Devazepide is a benzodiazepine derivative that interacts competitively with rat pancreatic CCK receptors as determined by Scatchard analysis against the specific binding of 125I-labelled CCK. In guinea-pig isolated ileum and colon, devazepide competitively blocked CCK-induced contractions with a potency greatly exceeding that of other non-peptide CCK antagonists such as proglumide, dibutyryl cyclic GMP and benzotript. It is confirmed that devazepide is a highly potent CCK-OP antagonist in this tissue. [4]
References:[1] Dickenson, John M., and Stephen J. Hill. "Synergistic interactions between human transfected adenosine A 1 receptors and endogenous cholecystokinin receptors in CHO cells."?European journal of pharmacology?302.1 (1996): 141-151.[2] Lavigne, G. J., W. R. Millington, and G. P. Mueller. "The CCK-A and CCK-B receptor antagonists, devazepide and L-365,260, enhance morphine antinociception only in non-acclimated rats exposed to a novel environment."Neuropeptides?21.2 (1992): 119-129.[3] Pu, Su-Fen, Hui-Xin Zhuang, and Ji-Sheng Han. "Cholecystokinin octapeptide (CCK-8) antagonizes morphine analgesia in nucleus accumbens of the rat via the CCK-B receptor."?Brain research?657.1 (1994): 159-164.[4] D"amato, M., I. F. Stamford, and A. Bennett. "Studies of three non‐peptide cholecystokinin antagonists (devazepide, lorglumide and loxiglumide) in human isolated alimentary muscle and guinea‐pig ileum."?British journal of pharmacology?102.2 (1991): 391-395.
