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盐酸格拉司琼

盐酸格拉司琼用途

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

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盐酸格拉司琼名称

[ CAS 号 ]:
107007-99-8

[ 中文名 ]:
盐酸格拉司琼

[ 英文名 ]:
Granisetron hydrochloride

[中文别名 ]:

格拉司琼盐酸盐

[英文别名 ]:

Granisetron hydrochloride
MFCD01747034
Granisetron HCl
Granisetron (Hydrochloride)

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 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

研究领域 >> 神经疾病

[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]

盐酸格拉司琼物理化学性质

[ 密度 ]:
1.33g/cm3

[ 沸点 ]:
532ºC at 760mmHg

[ 熔点 ]:
290-292°C

[ 分子式 ]:
C₁₈H₂₅ClN₄O

[ 分子量 ]:
348.870

[ 闪点 ]:
275.6ºC

[ 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

盐酸格拉司琼MSDS

盐酸格拉司琼毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NK7882200

CHEMICAL NAME :: 1H-Indazole-3-carboxamide, 1-methyl-N-(9-methyl-9-azabicyclo(3.3.1)non-3-yl)-, monohydrochloride, endo-

CAS REGISTRY NUMBER :: 107007-99-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C18-H24-N4-O.Cl-H

MOLECULAR WEIGHT :: 348.92

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 350 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Behavioral - muscle contraction or spasticity

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 350 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 3 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - tremor Gastrointestinal - nausea or vomiting

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4500 mg/kg/30D-I

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in leukocyte (WBC) count Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18200 mg/kg/26W-I

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in platelet count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 325 mg/kg/30D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Behavioral - tremor

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 52 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating - 19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 1500 mg/L

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6795,1990

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盐酸格拉司琼安全信息

[ 符号 ]:

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

盐酸格拉司琼合成路线

盐酸格拉司琼上下游产品

盐酸格拉司琼上游产品

盐酸格拉司琼下游产品

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。

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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

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...

更多文献

盐酸格拉司琼

盐酸格拉司琼用途

盐酸格拉司琼名称

盐酸格拉司琼生物活性

盐酸格拉司琼物理化学性质

盐酸格拉司琼MSDS

详细MSDS(安全技术说明书)

盐酸格拉司琼毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

盐酸格拉司琼安全信息

盐酸格拉司琼合成路线

详细合成路线

盐酸格拉司琼上下游产品

盐酸格拉司琼上游产品

盐酸格拉司琼下游产品

盐酸格拉司琼制备

盐酸格拉司琼海关

盐酸格拉司琼文献

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