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盐酸格拉司琼

盐酸格拉司琼

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?盐酸格拉司琼名称


















中文名

盐酸格拉司琼
英文名

Granisetron hydrochloride
中文别名


1-甲基-N-[内向-9-甲基-9-氮杂双环(3,3,1)壬烷-3-基]-lH-吲唑-3-甲酰胺盐酸盐




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N-(内-9-甲基-9-氮杂二环[3,3,1]壬-3-基)-吲哚-3-羧酰胺盐酸盐




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1-甲基-N-[内向-9-甲基-9-氮杂双环[3.3.1]壬烷-3-基]-1H-吲唑-3-甲酰胺盐酸盐




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格拉司琼盐酸盐




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桥-N-(9-甲基-9-氯杂二环[3.3.1]壬-3-基)-1-甲基-1H-吲唑-3-羧酰胺盐酸盐




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1-甲基-N-[(3-endo)-9-甲基-9-氮杂双环[3.3.1]壬-3-基]-1H-吲哚-3-甲酰胺盐酸盐



英文别名
更多





?盐酸格拉司琼生物活性












































描述
Granisetron(BRL 43694A)盐酸盐是5-HT3受体拮抗剂,可作为化疗后止吐剂。
相关类别




溶解度

体外:

在DMSO中10mM


储备液

1 mM 2.8664 mL 14.3320 mL 28.6640 mL
5 mM 0.5733 mL 2.8664 mL 5.7328 mL
10 mM 0.2866 mL 1.4332 mL 2.8664 mL


存储

粉末 -20℃下 3年
4℃下 2年
在溶剂中 -80℃下 6个月
-20℃下 1个月


运输

室温;可能会有所不同
SMILES

CN1N=C(C(N[C@H]2C[C@H](N3C)CCC[C@H]3C2)=O)C4=CC=CC=C41.[H]Cl
参考文献

[1]. Sanger GJ, Nelson DR. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur J Pharmacol. 1989 Jan 10;159(2):113-24.

[2]. Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou A, The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation. Int Immunopharmacol. 2010 Sep;10(9):1010-6.

[3]. Boccia RV, Gordan LN, Clark G, Efficacy and tolerability of transdermal granisetron for the control of chemotherapy-induced nausea and vomiting associated with moderately and highly emetogenic multi-day chemotherapy: a randomized, double-blind, phase III


相关活性
小分子




肉叶云香碱



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2-胺基-5-(4-硝基苯磺酰)-噻唑



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5-羟基色胺盐酸盐



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3-甲氧基-4-羟基肉桂酸钠



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盐酸硫利达嗪



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依匹哌唑



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利培酮



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TG6-10-1



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卡利拉嗪



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喹硫平



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舍吲哚



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1-(o-烯丙基苯氧基)-3-(异丙基氨基)-2-丙醇 盐酸盐



|

盐酸他利克索



|

凯他色林



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盐酸帕洛诺司琼






?盐酸格拉司琼物理化学性质














































密度 1.33g/cm3
沸点 532?C at 760mmHg
熔点 290-292°C
分子式 C18H25ClN4O
分子量 348.870
闪点 275.6?C
精确质量 348.171692
PSA 50.16000
LogP 3.44920
外观性状 白色至灰白色结晶固体
蒸汽压 0mmHg at 25°C
折射率 1.69
储存条件 Room temp
更多

1.性状:白色或微黄白色结晶性粉末,无臭。

2.熔点(℃):290-292。

3.溶解度:易溶于水,较难溶于甲醇,极难溶于乙醇,几不溶于乙醚。






?盐酸格拉司琼MSDS







?盐酸格拉司琼毒性和生态




盐酸格拉司琼毒性英文版






?盐酸格拉司琼安全信息




































符号

GHS07


GHS07
信号词
Warning
危害声明
H302
警示性声明
P301 + P312 + P330
个人防护装备
dust mask type N95 (US);Eyeshields;Faceshields;Gloves
危害码 (欧洲)
Xn: Harmful;Xi: Irritant;
风险声明 (欧洲)
R22
安全声明 (欧洲)
26-36-37
危险品运输编码 NONH for all modes of transport
RTECS号 NK7882200
海关编码 2933990090





?盐酸格拉司琼合成线路





















~%







盐酸格拉司琼结构式

盐酸格拉司琼

107007-99-8






文献:US4886808 A1, ;





~74%







盐酸格拉司琼结构式

盐酸格拉司琼

107007-99-8






文献:INKE, S.A. Patent: WO2008/151677 A1, 2008 ; Location in patent: Page/Page column 13 ;







?盐酸格拉司琼上下游产品













盐酸格拉司琼上游产品? 3

盐酸格拉司琼下游产品? 1







?盐酸格拉司琼制备


化合物(I)和化合物(Ⅱ)反应,即得格拉司琼。用氯化氢-乙醇酸化,得到盐酸格拉司琼。107007-99-8 preparation







?盐酸格拉司琼海关















海关编码 2933990090
中文概述 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素 品名, 成分含量, 用途, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%








?盐酸格拉司琼文献28

更多文献














Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude.

J. Neurosci. 35 , 9580-94, (2015)

Due to its distinct pharmacological profile and lower incidence of adverse events compared with other opioids, buprenorphine is considered a safe option for pain and substitution therapy. However, des…





In vitro percutaneous absorption enhancement of granisetron by chemical penetration enhancers.

Drug Dev. Ind. Pharm. 39(4) , 561-8, (2013)

Granisetron (GRN), a potent antiemetic agent, is frequently used to prevent nausea and vomiting induced by cancer cytotoxic chemotherapy and radiation therapy.As part of our efforts to further modify …





Comparison of the efficacy of ondansetron and granisetron to prevent postoperative nausea and vomiting after laparoscopic cholecystectomy: a systematic review and meta-analysis.

Surg. Laparosc. Endosc. Percutan. Tech. 23(1) , 79-87, (2013)

Our purpose was to assess the prophylactic antiemetic effects of ondansetron versus granisetron for laparoscopic cholecystectomy.We searched Medline, Cochrane Central Register of Controlled Trials, Pu…









?盐酸格拉司琼英文别名




























Granisetron hydrochloride


1-méthyl-N-[(3-endo)-9-méthyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide chlorhydrate


1H-Indazole-3-carboxamide, 1-methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-, hydrochloride (1:1)


1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide hydrochloride (1:1)


1H-indazole-3-carboxamide, 1-methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-, monohydrochloride


MFCD01747034


Granisetron HCl


1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3

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