Lubiprostone,136790-76-6

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YZ剂描述：

产品名称：Lubiprostone

产品别名：鲁比前列酮

英文别名：RU-0211;SPI-0211

靶点：ClC-2 chloride channels

CAS：136790-76-6

纯度：>98%

外观：白色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

在一项随机双盲的安慰剂对照研究中，用于ZLOIC的Lubiprostone24μgBID在慢性非癌症疼痛患者中是有效的和良好耐受的。 与安慰剂相比，用西洛膦ZL的患者的总体SBM反应率（主要终点）显著改善。 Lubiprostone表现出快速发作的效果，与安慰剂相比，早产4小时后，显着更多的患者报告了SBM。 这得到了一些次要分析的支持，包括在12周研究期间的应变，粪便一致性和便秘严重程度的统计学显着的整体改善。

溶解性：Ethanol ：72 mg/mL (184.4 mM)
DMSO ：72 mg/mL (184.4 mM)

体外研究：

Lubiprostone induces a robust secretory response in T84 monolayers. Lubiprostone induces a rise in cAMP levels that was sensitive to EP(4)-receptor blockage in T84 cells. Lubiprostone induces a contraction in rat and human stomach longitudinal muscle, which is inhibited by pretreatment with the EP(1) receptor antagonist but not by the EP(3) or EP(4) receptor antagonists. Lubiprostone also reduces electrically stimulated, neuronal contractions in rat and human colon circular muscle preparations. Lubiprostone (1 mM) stimulates higher elevations in TER despite lower I(sc) responses compared with the nonselective secretory agonist PGE(2) (1 mM). Lubiprostone significantly reduces mucosal-to-serosal fluxes of (3)H-labeled mannitol to levels comparable to those of normal control tissues and restored occludin localization to tight junctions. Lubiprostone causes comparable and maximal increases of I(sc) in T84 cells. Lubiprostone-induced increases in iodide efflux are ~80% of those obtained with forskolin. Lubiprostone activates Cl(-) secretion in T84 cells via cAMP, protein kinase A, and by increasing apical membrane CFTR protein. Lubiprostone, applied to the small intestinal mucosa in eight concentrations ranging from 1-3000 nM, evokes increases in Isc in a concentration-dependent manner with an EC50 of 42.5 nM. Lubiprostone applied to the mucosa of the colon in eight concentrations ranging from 1-3000 nM evokes increases in Isc in a concentration-dependent manner with an EC50 of 31.7 nM.

体内研究：Lubiprostone induces a CdCl(2)-insensitive secretory response in mouse intestine, but fail to induce intestinal Cl(-) secretion in Cftr-null mice.

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