同义名 :	利坦丝林 ;R 55667
	CAS号 :	87051-43-2
	货号 :	A189213
	分子式 :	C27H25F2N3OS
	纯度 :	99+%
	分子量 :	477.57
	MDL号 :	MFCD00069341
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Ritanserin is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors[3]. Ritanserin blocked CaV1.2 channel currents (ICa1.2) in a concentration-dependent manner (Kr = 3.61 µM); ICa1.2 inhibition was antagonized by Bay K 8644 and partially reverted upon washout. Conversely, the ritanserin analog ketanserin (100 µM) inhibited ICa1.2 by ~50%[4]. Ritanserin attenuates DGKα (Diacylglycerol kinase alpha) kinase activity while increasing the enzyme's affinity for ATP in vitro. In addition, R59022 and ritanserin function as DGKα inhibitors in cultured cells and activate protein kinase C (PKC)[5]. Ritanserin at doses of 1 and 3 mg/kg inhibited the development and expression of METH(methamphetamine)-induced behavioral sensitization in a dose-dependent manner. Furthermore, acute ritanserin inhibited METH challenge-induced increase in extracellular 5-HT but not DA levels in the prefrontal cortex[6].

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
NCT00000187	Cocaine-Related Disorders	Phase 2	Completed	-	United States, Pennsylvania ... 展开 >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 6178 收起 <<

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.09mL 0.42mL 0.21mL	10.47mL 2.09mL 1.05mL	20.94mL 4.19mL 2.09mL

参考文献

[1]Gaikwad U, Parle M, et al. Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7. [2]Johnson BA, Jasinski DR, et al. Ritanserin in the treatment of alcohol dependence--a multi-center clinical trial. Ritanserin Study Group. Psychopharmacology (Berl). 1996 Nov;128(2):206-15. [3]Leysen JE, Gommeren W, Van Gompel P, Wynants J, Janssen PF, Laduron PM. Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist. Mol Pharmacol. 1985 Jun;27(6):600-11 [4]Fusi F, Trezza A, Sgaragli G, Spiga O, Saponara S, Bova S. Ritanserin blocks CaV1.2 channels in rat artery smooth muscles: electrophysiological, functional, and computational studies. Acta Pharmacol Sin. 2020 Sep;41(9):1158-1166 [5]Boroda S, Niccum M, Raje V, Purow BW, Harris TE. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017 Jan 1;123:29-39 [6]Ago Y, Nakamura S, Kajita N, Uda M, Hashimoto H, Baba A, Matsuda T. Ritanserin reverses repeated methamphetamine-induced behavioral and neurochemical sensitization in mice. Synapse. 2007 Sep;61(9):757-63