|2-(4-(苯并[d][1,3]二氧戊环-5-基甲基)哌嗪-1-基)嘧啶|CsnPharm

CAS No.: 3605-01-4

Piribedil/双哌嘧啶 Catalog No. CSN18749

Synonyms: 吡贝地尔;双哌嘧啶

Piribedil is an antiparkinsonian agent and piperazine derivative which acts as a D2 and D3 receptor agonist.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Piribedil, the antiparkinsonian agent, showed comparable affinity for hα2A- (7.1) and hα2C- (7.2) adrenoceptors (ARs), whereas its affinity for hα2B-ARs was less marked (6.5). At a porcine α2A-AR-Gi1α-Cys351C (wild-type) fusion protein, piribedil competitively abolished (pA2=6.5) GTPase activity induced by epinephrine. piribedil showed only modest affinity for rat α1-ARs (5.9) and weakly antagonized NE-induced activation of phospholipase C via hα1A-ARs (pKb=5.6). Furthermore, piribedil (2.5–4.0 mg/kg s.c.) accelerated hippocampal NE(norepinephrine) synthesis, elevated dialysis levels of NE in hippocampus and frontal cortex, and blocked hypnotic-sedative properties of the α2-AR agonist xylazine
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
NCT00727727	-	-	Completed	-	Germany ... more >> Medical Practice for Neurology Dresden, Germany, 01307 Medical Practice for Neurology Wedel, Germany, 22880 Collapse <<
NCT00725478	-	-	Completed	-	-
NCT01519856	-	-	Completed	-	Germany ... more >> Dr. Erich Scholz Boeblingen, Baden-Wuertemberg, Germany, 71034 Collapse <<

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参考文献

[1] Millan MJ, Cussac D, et al. Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization. J Pharmacol Exp Ther. 2001 Jun;297(3):876-87.
[2] Neumann S, Huang W, et al. A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. Endocrinology. 2010 Jul;151(7):3454-9.

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
- 3.3519 mL
- 16.7594 mL
- 33.5188 mL
- 5 mM
- 0.6704 mL
- 3.3519 mL
- 6.7038 mL
- 10 mM
- 0.3352 mL
- 1.6759 mL
- 3.3519 mL

技术信息

CAS号

3605-01-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H18N4O2

运输

蓝冰

分子量

298.34

别名

吡贝地尔;双哌嘧啶

溶解度

DMSO	59.0 mg/mL (197.8 mM)
Water	Insoluble
Ethanol	58.0 mg/mL (194.4 mM)

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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

NCT00727727	-	-	Completed	-	Germany ... more >> Medical Practice for Neurology Dresden, Germany, 01307 Medical Practice for Neurology Wedel, Germany, 22880 Collapse <<
NCT00725478	-	-	Completed	-	-
NCT01519856	-	-	Completed	-	Germany ... more >> Dr. Erich Scholz Boeblingen, Baden-Wuertemberg, Germany, 71034 Collapse <<
NCT00591994	Tinnitus	Not Applicable	Completed	-	Brazil ... more >> OTOSUL,Otorrinolaringologia Sul-Fluminense Volta Redonda, RJ, Brazil, 27255-650 Collapse <<
NCT01007864	Idiopathic Parkinson's Disease	Phase 3	Completed	-	Germany ... more >> Ulm, Baden-Württemberg, Germany, 89081 Wolfach, Baden-Württemberg, Germany, 77709 München, Bayern, Germany, 80804 Berlin-Steglitz, Berlin, Germany, 12163 Marburg, Hessen, Germany, 35043 Göttingen, Niedersachsen, Germany, 37075 Dresden, Sachsen, Germany, 01307 Leipzig, Sachsen, Germany, 04107 Gera, Thüringen, Germany, 07551 Stadtroda, Thüringen, Germany, 07646 Berlin, Germany, 12200 Berlin, Germany, 13353 Collapse <<

Piribedil/双哌嘧啶 Catalog No. CSN18749

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