盐酸曲林菌素

盐酸曲林菌素用途

Trequinsin hydrochloride (HL 725) 是高效的血小板 CAMP 磷酸二酯酶 (PDE)的抑制剂,IC50的0.25 nM。Trequinsin hydrochloride (HL 725) 是 ADP、胶原蛋白、凝血酶和肾上腺素在体外诱导的血小板聚集的极有效抑制剂。

盐酸曲林菌素名称

[ CAS 号 ]:
78416-81-6

[ 中文名 ]:
盐酸曲林菌素

[ 英文名 ]:
Trequinsin hydrochloride

[中文别名 ]:

曲喹辛

[英文别名 ]:

trequinsine
HL 725 HCL
TREQUINSIN HYDROCHLORIDE MINIMUM
TREQUINSIN HYDROCHLORIDE
Trequinsin,HCl
HL 725

盐酸曲林菌素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 代谢疾病

[体外研究]

盐酸特雷奎因除了具有心血管和抗高血压作用外,还具有非常强的抗血小板活性[1]。盐酸特雷奎因是[Ca2+]i[3]的有效激动剂。【2010年世界卫生组织志愿者精子活力测定标准：与正常精子细胞活力测定标准一致】。浓度：10μM,孵育时间：20min。结果：引起[Ca2+]i浓度依赖性增加(EC50=6.4μM[95%可信区间(CI)：4.1-9.9μM]。

[参考文献]

[1]. D Ruppert,, et al. HL 725, an extremely potent inhibitor of platelet phosphodiesterase and induced platelet aggregation in vitro. Life Sci. 1982 Nov 8;31(19):2037-43.

[2]. K C Agarwal, et al. Role of plasma adenosine in the antiplatelet action of HL 725, a potent inhibitor of cAMP phosphodiesterase: species differences. Thromb Res. 1987 Jul 15;47(2):191-200.

[3]. Rachel C McBrinn, et al. Novel pharmacological actions of trequinsin hydrochloride improve human sperm cell motility and function. Br J Pharmacol. 2019 Dec;176(23):4521-4536.

盐酸曲林菌素物理化学性质

[ 沸点 ]:
613.8ºC at 760 mmHg

[ 分子式 ]:
C₂₄H₂₈ClN₃O₃

[ 分子量 ]:
441.95000

[ 闪点 ]:
325ºC

[ 精确质量 ]:
441.18200

[ PSA ]:
57.75000

[ LogP ]:
4.38670

[ 储存条件 ]:
2-8°C，干燥，密封

盐酸曲林菌素MSDS

盐酸曲林菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UW7727000

CHEMICAL NAME :: 4H-Pyrimido(6,1-a)isoquinolin-4-one, 2,3,6,7-tetrahydro-9,10-dimethoxy-3-methyl- 2-((2,4,6-trimethylphenyl)imino)-, monohydrochloride

CAS REGISTRY NUMBER :: 78416-81-6

LAST UPDATED :: 198803

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C24-H27-N3-O3.Cl-H

MOLECULAR WEIGHT :: 442.00

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

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

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 27,1470,1984

盐酸曲林菌素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UW7727000

盐酸曲林菌素合成路线

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盐酸曲林菌素文献

Pituitary adenylate cyclase activating polypeptide (PACAP) potently enhances tyrosine hydroxylase (TH) expression in adrenal chromaffin cells.

Life Sci. 54(22) , 1735-43, (1994)

In primary cultured bovine adrenal chromaffin cells (BACC), pituitary adenylate cyclase activating polypeptide 1-38 (PACAP) produced a dose related increase in tyrosine hydroxylase (TH) Vmax when meas...

Atrial natriuretic peptide reduces cyclic AMP by activating cyclic GMP-stimulated phosphodiesterase in vascular endothelial cells.

J. Cardiovasc. Pharmacol. 24(3) , 351-7, (1994)

Bovine aortic endothelial cells contain cyclic GMP-stimulated phosphodiesterase (PDE) regulating intracellular cyclic AMP and cyclic GMP levels. To investigate the roles of this PDE isoform for cyclic...

Role of cGMP-inhibited phosphodiesterase and sarcoplasmic calcium in mediating the increase in basal heart rate with nitric oxide donors.

J. Mol. Cell. Cardiol. 32(10) , 1831-40, (2000)

Nitric oxide (NO) donors increase heart rate (HR) through a guanylyl cyclase-dependent stimulation of the pacemaker current I(f), without affecting basal I(Ca-L). The activity of I(f)is known to be en...

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