< 生产厂家价格 >

盐酸他利克索

盐酸他利克索用途

B-HT 920(Talipexole 2Hcl)是多巴胺D2受体和α2-肾上腺素受体激动剂,5-HT3受体拮抗剂,有抗帕金森病活性。

点击显示

盐酸他利克索名称

[ CAS 号 ]:
36085-73-1

[ 中文名 ]:
他利克索

[ 英文名 ]:
B-HT 920

[中文别名 ]:

盐酸他利克索

[英文别名 ]:

B-HT 920 dihydrochloride
Talipexoledihydrochloride
Domin
Talipexole
B-HT 920
MFCD00274573

盐酸他利克索生物活性

[ 描述 ]:

B-HT 920(Talipexole 2Hcl)是多巴胺D2受体和α2-肾上腺素受体激动剂,5-HT3受体拮抗剂,有抗帕金森病活性。

[ 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

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[参考文献]

[1]. Ricci and Taira Adrenoceptor involvement in the cardiovascular responses to B-HT 920 in sinoaortic denervated rats. Gen.Pharmacol. (1999)32 29.

[2]. Eur J Pharmacol. 1997 May 1;325(2-3):137-44.

[3]. Kohno Y, Fukuzaki K, Kitahara K, Koja T.Anti-tremor activity of talipexole produced by selective dopamine D2 receptor stimulation in cynomolgus monkeys with unilateral lesions in the ventromedial tegmentum.Eur J Pharmacol. 1997 Jan 29;319(2-3):197-205.

[4]. Momiyama T, Sasa M, Takaori S.Inhibition by talipexole, a thiazolo-azepine derivative, of dopaminergic neurons in the ventral tegmental area.Life Sci. 1991;49(7):535-43.

[5]. Nishikawa T, Yamada S, Tsuda A, Tanaka M, Koga I, Uchida Y.Chronic treatment with talipexole dihydrochloride on abnormal involuntary movement in humans.Clin Neuropharmacol. 1990 Jun;13(3):259-63.

[6]. Robertson, G.S., et al., In vivo comparisons of the effects of quinpirole and the putative presynaptic dopaminergic agonists B-HT 920 and SND 919 on striatal dopamine and acetylcholine release. J Pharmacol Exp Ther, 1993. 264(3): p. 1344-51.

[相关活性小分子]

盐酸他利克索物理化学性质

[ 沸点 ]:
364.6ºC at 760mmHg

[ 熔点 ]:
245ºC dec.

[ 分子式 ]:
C₁₀H₁₇Cl₂N₃S

[ 分子量 ]:
282.233

[ 闪点 ]:
174.3ºC

[ 精确质量 ]:
281.052032

[ PSA ]:
70.39000

[ LogP ]:
3.43500

[ 外观性状 ]:
淡黄色固体

[ 储存条件 ]:
室温，干燥

盐酸他利克索MSDS

详细MSDS(安全技术说明书)

盐酸他利克索毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ7050340

CHEMICAL NAME :: 4H-Thiazolo(4,5-d)azepin-2-amine, 5,6,7,8-tetrahydro-6-(2-propenyl)-, dihydrochloride

CAS REGISTRY NUMBER :: 36085-73-1

LAST UPDATED :: 199712

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C10-H15-N3-S.2Cl-H

MOLECULAR WEIGHT :: 282.26

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 :: 403 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - chromodacryorrhea Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - tremor

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 66 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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 455 mg/kg

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

REFERENCE :: GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2820808

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >32 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - coma

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,401,1993 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 mg/kg/13W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Reproductive - Effects on Newborn - stillbirth

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 364 mg/kg/52W-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - changes in lung weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - changes in prostate weight

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,383,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 728 mg/kg/52W-I

TOXIC EFFECTS :: Blood - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 45,545,1993 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5600 ug/kg

SEX/DURATION :: female 14 day(s) pre-mating - 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,9,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3300 ug/kg

SEX/DURATION :: female 7-17 day(s) after conception

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,9,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 42 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 46,9,1993

点击显示

盐酸他利克索安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3.0

[ RTECS号 ]:
XJ7050340

[ 海关编码 ]:
2934999090

盐酸他利克索海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸他利克索文献

Duration of drug action of dopamine D2 agonists in mice with 6-hydroxydopamine-induced lesions.

Neuroreport 26 , 1126-32, (2015)

Although 6-hydroxydopamine-induced (6-OHDA-induced) rats are a well-known Parkinson's disease model, the effects of dopamine D2 agonists in mice with 6-OHDA-induced lesions are not completely understo...

Mechanism of decongestant activity of alpha 2-adrenoceptor agonists.

Pulm. Pharmacol. Ther. 21(3) , 449-54, (2008)

The vascular bed in nasal mucosa of different species, including human, is highly vascularized and an extensive sinusoidal network of large capacitance vessels is present deep within the submucosa. Wh...

Paraquat leads to dopaminergic neural vulnerability in organotypic midbrain culture.

Neurosci. Res. 46(4) , 523-32, (2003)

Paraquat (1,1'-dimethyl-4,4'-bipyridinium, PQ) is a herbicide to possibly induce Parkinson's disease (PD), since a strong correlation has been found between the incidence of the disease and the amount...

更多文献