中文名 | CGP71683 hydrochloride |
英文名 | CGP71683 hydrochloride |
别名 | 盐酸CGP71683 N-[[反式-4-[[(4-氨基-2-喹唑啉基)氨基]甲基]环己基]甲基]-1-萘磺酰胺盐酸盐 N-(((1R,4R)-4-(((4-氨基喹唑啉-2-基)氨基)甲基)环己基)甲基)萘-1-磺酰胺盐酸盐 |
英文别名 | CGP 71683 CGP-71683A CGP71683A CGP71683HCl 192322-50-2 CGP 71683A UNII-45B73P82A3 UNII-45B73P82A3 CGP71683 hydrochloride CGP 71683 HYDROCHLORIDE CGP 71683A hydrochloride N-[[TRANS-4-[[(4-AMINO-2-QUINAZOLINYL)AMINO]METHYL]CYCLOHEXYL]METHYL]-1-NAPHTHALENESULFONAMIDE HYDROCHLORIDE |
CAS | 192322-50-2 |
化学式 | C26H30ClN5O2S |
分子量 | 512.07 |
溶解度 | H2O: ~ 14mg/ml,可溶 |
存储条件 | Inert atmosphere,2-8°C |
外观 | 固体 |
颜色 | off-white |
体外研究 | CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a K i of 1.3 nM, and shows no obvious activity at Y1 receptor (K i , >4000 nM) and Y2 receptor (K i , 200 nM) in cell membranes. |
体内研究 | CGP71683 (15 nmol/rat, icv, twice daily) shows anorexigenic effect, reducing food intake and bady weight of fed rats. CGP71683 causes 3-times higher serum total T4 and 37% increase in free T4 in the fasted rats than in the fasted controls rats. |
安全术语 | 24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 3 |
参考资料 展开查看 | 1: Ghahramanian Golzar M, Babri S, Ataie Z, Ebrahimi H, Mirzaie F, Mohaddes G. NPY Receptors Blockade Prevents Anticonvulsant Action of Ghrelin in the Hippocampus of Rat. Adv Pharm Bull. 2013;3(2):265-71. doi: 10.5681/apb.2013.043. Epub 2013 Aug 20. PubMed PMID: 24312846; PubMed Central PMCID: PMC3848244. 2: Li L, Mayer M, Schneider E, Schreiber E, Bernhardt G, Peng S, Buschauer A. Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: analogues of the quinazoline-type anti-obesity Y5 antagonist CGP 71683A. Arch Pharm (Weinheim). 2003 Dec;336(12):585-90. PubMed PMID: 14677152. 3: Lecklin A, Lundell I, Paananen L, Wikberg JE, Männistö PT, Larhammar D. Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br J Pharmacol. 2002 Apr;135(8):2029-37. PubMed PMID: 11959807; PubMed Central PMCID: PMC1573328. 4: Della Zuana O, Sadlo M, Germain M, Félétou M, Chamorro S, Tisserand F, de Montrion C, Boivin JF, Duhault J, Boutin JA, Levens N. Reduced food intake in response to CGP 71683A may be due to mechanisms other than NPY Y5 receptor blockade. Int J Obes Relat Metab Disord. 2001 Jan;25(1):84-94. PubMed PMID: 11244462. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.953 ml | 9.764 ml | 19.529 ml |
5 mM | 0.391 ml | 1.953 ml | 3.906 ml |
10 mM | 0.195 ml | 0.976 ml | 1.953 ml |
5 mM | 0.039 ml | 0.195 ml | 0.391 ml |
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