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Arazasetron

编号: 20535
Cas号: 2025360-90-9
纯度: 98% Min.

Arazasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27.

仅供研究使用。 我们不向患者出售。

化学信息

名称Arazasetron
Iupac 化学名称N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide
同义词R-Azasetron; Azasetron, R; 61JC7L0Q4O; 2025360-90-9; UNII-61JC7L0Q4O
英文同义词R-Azasetron; Azasetron, R; 61JC7L0Q4O; 2025360-90-9; UNII-61JC7L0Q4O
分子式C17H20ClN3O3
分子量349.81
SmileO=C(C1=C(OCC(N2C)=O)C2=CC(Cl)=C1)N[C@H]3CN4CCC3CC4
InChiKeyWUKZPHOXUVCQOR-ZDUSSCGKSA-N
InChiInChI=1S/C17H20ClN3O3/c1-20-14-7-11(18)6-12(16(14)24-9-15(20)22)17(23)19-13-8-21-4-2-10(13)3-5-21/h6-7,10,13H,2-5,8-9H2,1H3,(H,19,23)/t13-/m0/s1
Cas号2025360-90-9
相关CAS号

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包装价格库存纯度备货期
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外观性状固体粉末
纯度98% Min.
存储短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度
可溶性溶于DMSO
处理方式
运输条件作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周.
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

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PubMed PMID: 28373467. 4: Koshiyama M, Matsumura N, Imai S, Yamanoi K, Abiko K, Yoshioka Y, Yamaguchi K, Hamanishi J, Baba T, Konishi I. Combination of Aprepitant, Azasetron, and Dexamethasone as Antiemetic Prophylaxis in Women with Gynecologic Cancers Receiving Paclitaxel/Carboplatin Therapy. Med Sci Monit. 2017 Feb 15;23:826-833. PubMed PMID: 28198358; PubMed Central PMCID: PMC5322867. 5: Chen FC, Wang LH, Guo J, Shi XY, Fang BX. Simultaneous Determination of Dexamethasone, Ondansetron, Granisetron, Tropisetron, and Azasetron in Infusion Samples by HPLC with DAD Detection. J Anal Methods Chem. 2017;2017:6749087. doi: 10.1155/2017/6749087. Epub 2017 Jan 11. PubMed PMID: 28168082; PubMed Central PMCID: PMC5266853. 6: Tanaka T, Ago Y, Umehara C, Imoto E, Hasebe S, Hashimoto H, Takuma K, Matsuda T. Role of Prefrontal Serotonergic and Dopaminergic Systems in Encounter-Induced Hyperactivity in Methamphetamine-Sensitized Mice. 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Synergistic effect between prelimbic 5-HT3 and CB1 receptors on memory consolidation deficit in adult male Sprague-Dawley rats: An isobologram analysis. Neuroscience. 2016 Mar 11;317:173-83. doi: 10.1016/j.neuroscience.2015.12.010. Epub 2015 Dec 14. PubMed PMID: 26701293. 11: Hasebe S, Ago Y, Nishiyama S, Oka S, Hashimoto H, Takuma K, Matsuda T. Pharmacological profile of encounter-induced hyperactivity in isolation-reared mice. Behav Pharmacol. 2015 Oct;26(7 Spec No):681-90. doi: 10.1097/FBP.0000000000000140. PubMed PMID: 25932719. 12: Nasehi M, Kafi F, Khakpai F, Zarrindast MR. Involvement of the serotonergic system of the ventral hippocampus (CA3) on amnesia induced by ACPA in mice. Behav Brain Res. 2015 Jun 1;286:356-63. doi: 10.1016/j.bbr.2015.03.011. Epub 2015 Mar 11. PubMed PMID: 25771207. 13: Liu J, Tan L, Zhang H, Li H, Liu X, Yan Z, Chen J, Yang H, Zhang D. QoL evaluation of olanzapine for chemotherapy-induced nausea and vomiting comparing with 5-HT3 receptor antagonist. Eur J Cancer Care (Engl). 2015 May;24(3):436-43. doi: 10.1111/ecc.12260. Epub 2014 Nov 18. PubMed PMID: 25404537. 14: Lee HY, Kim HK, Lee KH, Kim BS, Song HS, Yang SH, Kim JH, Kim YH, Kim JG, Kim SW, Kim DW, Kim SY, Park HS. A Randomized Double-Blind, Double-Dummy, Multicenter Trial of Azasetron versus Ondansetron to Evaluate Efficacy and Safety in the Prevention of Delayed Nausea and Vomiting Induced by Chemotherapy. Cancer Res Treat. 2014 Jan;46(1):19-26. doi: 10.4143/crt.2014.46.1.19. Epub 2014 Jan 15. PubMed PMID: 24520219; PubMed Central PMCID: PMC3918522. 15: Nakamura H, Yokoyama H, Takayanagi R, Yoshimoto K, Nakajima A, Okuyama K, Iwase O, Yamada Y. Theoretical evaluation of antiemetic effects of 5-HT3 receptor antagonists for prevention of vomiting induced by cisplatin. Eur J Drug Metab Pharmacokinet. 2015 Mar;40(1):39-44. doi: 10.1007/s13318-014-0175-z. Epub 2014 Jan 28. PubMed PMID: 24470169. 16: Bell R, Duke AA, Gilmore PE, Page D, Bègue L. Anxiolytic-like effects observed in rats exposed to the elevated zero-maze following treatment with 5-HT2/5-HT3/5-HT4 ligands. Sci Rep. 2014 Jan 24;4:3881. doi: 10.1038/srep03881. PubMed PMID: 24457553; PubMed Central PMCID: PMC5379192. 17: Hiramatsu N, Ago Y, Hasebe S, Nishimura A, Mori K, Takuma K, Matsuda T. Synergistic effect of 5-HT1A and σ1 receptor activation on prefrontal dopaminergic transmission under circulating steroid deficiency. Neuropharmacology. 2013 Dec;75:53-61. doi: 10.1016/j.neuropharm.2013.06.026. Epub 2013 Jul 9. PubMed PMID: 23851260. 18: Endo J, Iihara H, Yamada M, Yanase K, Kamiya F, Ito F, Funaguchi N, Ohno Y, Minatoguchi S, Itoh Y. A randomized controlled non-inferiority study comparing the antiemetic effect between intravenous granisetron and oral azasetron based on estimated 5-HT3 receptor occupancy. Anticancer Res. 2012 Sep;32(9):3939-47. PubMed PMID: 22993341. 19: Sun L, Cun D, Yuan B, Cui H, Xi H, Mu L, Chen Y, Liu C, Wang Z, Fang L. Formulation and in vitro/in vivo correlation of a drug-in-adhesive transdermal patch containing azasetron. J Pharm Sci. 2012 Dec;101(12):4540-8. doi: 10.1002/jps.23317. Epub 2012 Sep 12. PubMed PMID: 22972714. 20: Ortega JE, Mendiguren A, Pineda J, Meana JJ. Regulation of central noradrenergic activity by 5-HT(3) receptors located in the locus coeruleus of the rat. Neuropharmacology. 2012 Jun;62(8):2472-9. doi: 10.1016/j.neuropharm.2012.02.018. Epub 2012 Mar 1. PubMed PMID: 22401957.

化学结构

20535 - Arazasetron | CAS 2025360-90-9

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