|3-(2-(4-(4-氟苯甲酰基)哌啶-1-基)乙基)喹唑啉-2,4(1H,3H)-二酮 (2R,3R)-2,3-二羟基琥珀酸盐|CsnPharm

CAS No.: 83846-83-7

酒石酸酮色啉盐 Catalog No. CSN11251

Synonyms: R41468 tartrate;Ketanserin (tartrate);KJK-945

Ketanserin Tartrate is a water soluble selective 5-HT2A and 5-HT1D antagonist.

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生物活性

实验方案

技术信息

生物活性

描述Ketanserin tartrate, a kind of antihypertensive drugs, is a selective 5HT2 serotonergic receptor antagonist and can antagonize the alpha 1-adrenergic receptor at high concentrations. In vitro studies, ketanserin tartrate, with a concentration up to 300 ng/ml, could decrease the 3-hydroxy, 3-methylglutaryl coenzyme A (HMG CoA) reductase activity in cultured human skin fibroblasts, when incubated with cells for 14h^[3]. In vivo studies, it was found that ketanserin tartrate could antagonize the systemic and regional hemodynamic effects of serotonin and cirazoline but not of UK-14,304, as well as antagonize serotonin and cirazoline, homogeneously in all vascular beds^[4]. Besides this, ketanserin tartrate contributed to the decreases of systolic and diastolic blood pressure in patients with mild or moderate hypertension, when given 20 to 60 mg daily for 12 weeks, while not alter heart rate^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01778686	Healthy	Not Applicable	Completed	-	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Copenhagen, Denmark, 2100 Collapse <<
NCT03321136	Healthy	Early Phase 1	Recruiting	March 2019	Switzerland ... more >> University Hospital Recruiting Basel, Switzerland, 4031 Contact: Matthias E Liechti, Prof. Dr. med. matthias.liechti@usb.ch Contact: Friederike Holze, MSc friederike.holze@usb.ch Collapse <<
NCT03289949	Basic Science	Phase 1	Recruiting	December 31, 2019	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Recruiting Copenhagen, Denmark, 2100 Contact: Gitte M Knudsen, Professor Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8331 mL
- 9.1657 mL
- 18.3313 mL
- 5 mM
- 0.3666 mL
- 1.8331 mL
- 3.6663 mL
- 10 mM
- 0.1833 mL
- 0.9166 mL
- 1.8331 mL

技术信息

CAS号

83846-83-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H28FN3O9

运输

蓝冰

分子量

545.51

别名

R41468 tartrate;Ketanserin (tartrate);KJK-945;R-49945

溶解度

DMSO	145.0 mg/mL (265.8 mM) warming
Water	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01778686	Healthy	Not Applicable	Completed	-	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Copenhagen, Denmark, 2100 Collapse <<
NCT03321136	Healthy	Early Phase 1	Recruiting	March 2019	Switzerland ... more >> University Hospital Recruiting Basel, Switzerland, 4031 Contact: Matthias E Liechti, Prof. Dr. med. matthias.liechti@usb.ch Contact: Friederike Holze, MSc friederike.holze@usb.ch Collapse <<
NCT03289949	Basic Science	Phase 1	Recruiting	December 31, 2019	Denmark ... more >> Neurobiology Research Unit, Rigshospitalet Recruiting Copenhagen, Denmark, 2100 Contact: Gitte M Knudsen, Professor Collapse <<
NCT00557219	Acute Renal Failure	Phase 3	Terminated(Main cooperator fin... more >>ished cooperation) Collapse <<	-	Poland ... more >> Department of Cardiac Anesthesiology, Medical University of Gdańsk Gdańsk, Poland, 80-211 Collapse <<
NCT02451072	Healthy	Not Applicable	Completed	-	Switzerland ... more >> Center for Psychiatric Research, Department of Psychiatry, Psychotherapy and Psychosomatic, Psychiatric Hospital, University of Zurich Zurich, Switzerland, 8032 Collapse <<
NCT02632877	Diabetic Foot Ulcer	Phase 1 Phase 2	Completed	-	Mexico ... more >> Molecular Biology and Gene Therapy Institute Guadalajara, Jalisco, Mexico, 44340 Hospital Valentín Gómez Farías Zapopan, Jalisco, Mexico Collapse <<
NCT03646318	Critical Illness	Phase 4	Not yet recruiting	May 1, 2019	-
NCT01329887	Severe Sepsis ... more >> Septic Shock Collapse <<	Phase 3	Completed	-	Netherlands ... more >> Medical Centre Leeuwarden Leeuwarden, Netherlands Collapse <<

酒石酸酮色啉盐 Catalog No. CSN11251

靶点选择性

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