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倍他司汀

倍他司汀用途

Betahistine 是一种具有口服活性的的组胺 H1 受体 (histamine H1 receptor) 激动剂和 H3 受体 (H3 receptor) 的拮抗剂。Betahistine 可以用于类风湿性关节炎 (RA) 的研究。

倍他司汀名称

[ CAS 号 ]:
5638-76-6

[ 中文名 ]:
2-(2-甲基氨基乙基)吡啶

[ 英文名 ]:
Betahistine

[中文别名 ]:

[英文别名 ]:

2-(b-Methylaminoethyl)pyridine
N-methyl-2-pyridin-2-ylethanamine
Pyridine, 2-[2- (methylamino)ethyl]-
MFCD00006362
N-Methyl-2-(2-pyridinyl)ethanamine
EINECS 227-086-4
Suzutolon
2-Pyridineethanamine, N-methyl-
2-(2-Methylaminoethyl)pyridine
N-methyl-2-(pyridin-2-yl)ethanamine

倍他司汀生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H1 Receptor

H3 receptor

[体外研究]

倍他司汀(0～10μM)可抑制[125I]碘氧自由基与CHO(rH3(445)R)和CHO(hH3(445)R)细胞膜的结合,IC50分别为1.9μM和3.3μM。Ki值分别为1.4μM和2.5μM[2]。倍他司汀(0～10μM)对CHO(rH3(445)R)、CHO(rH3(413)R)和CHO(hH3(445)R)细胞cAMP的形成具有调节作用。低浓度时,倍他司汀表现为明显的反激动剂,并逐渐增强cAMP的形成,EC50值分别为0.1nm、0.05nm和0.3nm。相反,当浓度高于10nm时,倍他司汀抑制cAMP的形成,CHO(rH3(445)R)的EC50值为0.1μM,激动剂活性完全[2]。

[体内研究]

倍他司汀(腹腔或口服给药；0.1-30mg/kg；单次给药)急性给药后,远端甲基组胺(t-MeHA)水平增加,ED50为0.4mg/kg,显示出相反的痛苦。此外,急性口服给药后,雄性Swissmice的t-MeHA水平增加,ED50为2 mg/kg[2]。倍他司汀(口服；1和5mg/kg；每天3周)可减轻关节炎的严重程度,并降低CIA小鼠足组织中促炎细胞因子的水平[3]。动物模型：胶原诱导关节炎(CIA)DBA/1雄性小鼠模型[3]剂量：1mg/kg；5mg/kg给药：口服；诱导21d后第21天至第42天结果：通过减少关节破坏改善小鼠CIA。

[参考文献]

[1]. Poyurovsky M, et al. The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3.

[2]. Gbahou F, et al. Effects of betahistine at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54.

[3]. Tang KT, et al. Betahistine attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245.

倍他司汀物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
210.9±15.0 °C at 760 mmHg

[ 分子式 ]:
C₈H₁₂N₂

[ 分子量 ]:
136.194

[ 闪点 ]:
96.7±0.0 °C

[ 精确质量 ]:
136.100052

[ PSA ]:
24.92000

[ LogP ]:
0.10

[ 外观性状 ]:
淡黄色

[ 蒸汽压 ]:
0.2±0.4 mmHg at 25°C

[ 折射率 ]:
1.510

[ 储存条件 ]:
-20℃

倍他司汀MSDS

详细MSDS(安全技术说明书)

倍他司汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UT5552000

CHEMICAL NAME :: Pyridine, 2-(2-(methylamino)ethyl)-

CAS REGISTRY NUMBER :: 5638-76-6

BEILSTEIN REFERENCE NO. :: 0112294

LAST UPDATED :: 199701

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C8-H12-N2

MOLECULAR WEIGHT :: 136.22

WISWESSER LINE NOTATION :: T6NJ B2M1

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 :: 6110 mg/kg

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

REFERENCE :: PBFMAV Problemi na Farmatsiyata. Problems in Pharmacy. (Durzhavno Izdatel'stvo Meditsina i Fizkultura, Pl. Slaveikov II, Sofia, Bulgaria) V.1- 1973- Volume(issue)/page/year: 13,63,1985

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 980 mg/kg

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

REFERENCE :: PBFMAV Problemi na Farmatsiyata. Problems in Pharmacy. (Durzhavno Izdatel'stvo Meditsina i Fizkultura, Pl. Slaveikov II, Sofia, Bulgaria) V.1- 1973- Volume(issue)/page/year: 13,63,1985

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2920 mg/kg

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

REFERENCE :: PBFMAV Problemi na Farmatsiyata. Problems in Pharmacy. (Durzhavno Izdatel'stvo Meditsina i Fizkultura, Pl. Slaveikov II, Sofia, Bulgaria) V.1- 1973- Volume(issue)/page/year: 13,63,1985

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 320 mg/kg

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

REFERENCE :: PBFMAV Problemi na Farmatsiyata. Problems in Pharmacy. (Durzhavno Izdatel'stvo Meditsina i Fizkultura, Pl. Slaveikov II, Sofia, Bulgaria) V.1- 1973- Volume(issue)/page/year: 13,63,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 94500 mg/kg/90D-C

TOXIC EFFECTS :: Behavioral - muscle weakness Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,344,1968

倍他司汀安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;C: Corrosive;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S37/39

[ 危险品运输编码 ]:
UN2735

[ WGK德国 ]:
2

[ RTECS号 ]:
UT5552000

[ 海关编码 ]:
2933399090

倍他司汀合成路线

详细合成路线

倍他司汀上下游产品

倍他司汀上游产品

倍他司汀下游产品

倍他司汀海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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 ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

倍他司汀文献

Development of novel sustained release matrix pellets of betahistine dihydrochloride: effect of lipophilic surfactants and co-surfactants.

Pharm. Dev. Technol. 17(5) , 583-93, (2012)

Sustained release matrix pellets of the freely water soluble drug, betahistine dihydrochloride (BH), were prepared using freeze pelletization technique. Different waxes and lipids (cetyl alcohol, bees...

Comparison of the therapeutic efficacy of a fixed low-dose combination of cinnarizine and dimenhydrinate with betahistine in vestibular neuritis: a randomized, double-blind, non-inferiority study.

Clin. Drug Investig. 32(6) , 387-99, (2012)

Vestibular neuritis (VN) is a strongly disabling disease of the peripheral vestibular system. Rapid and effective relief of symptoms is important to allow patients to promptly return to normal physica...

Betahistine or Cinnarizine for treatment of Meniere's disease.

Med. Arh. 66(6) , 396-8, (2012)

Meniere's disease is a condition with sudden attacks of vertigo with nausea and vomiting accompanied by loss of hearing and buzzing sensation in the ears, most commonly unilateral. The exact cause of ...

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