產(chǎn)品說(shuō)明

該產(chǎn)品包含在以下化合物庫(kù)中:

質(zhì)量控制

• 純度 = 98.00%

化學(xué)性質(zhì)

?

實(shí)驗(yàn)操作

產(chǎn)品描述

H-1152，異喹啉磺衍生物，是Rho激酶的高效、選擇性、膜透過(guò)性抑制劑，其Ki值為1.6 nM，與對(duì)其它絲氨酸/蘇氨酸激酶相比具有高度選擇性。

在人神經(jīng)畸胎瘤細(xì)胞(NT-2)中，H-1152以劑量依賴的方式阻斷溶血磷脂酸(LPA)誘導(dǎo)的豆蔻?；槐彼酑激酶底物(MARCKS)磷酸化，其IC50值為2.5 μM[1]。

H-1152處理的人小梁細(xì)胞（HTM）表現(xiàn)出細(xì)胞伸長(zhǎng)和分離、退化、黏著斑以及肌動(dòng)蛋白應(yīng)力纖維缺失。H-1152處理大鼠眼睛顯著降低其眼內(nèi)壓(IOP)，擴(kuò)大細(xì)胞間隙，減少TM近微管區(qū)域的胞外物質(zhì)[2]。

在出生后小鼠螺旋神經(jīng)節(jié)的分離培養(yǎng)物中，H-1152能提高神經(jīng)節(jié)的長(zhǎng)度。但H-1152對(duì)不同神經(jīng)元形態(tài)比率或神經(jīng)元存活變化的減少?zèng)]有影響[3]。

H-1152使苯腎上腺素(PE)曲線向右改變，而對(duì)電場(chǎng)刺激(EFS)誘導(dǎo)的收縮沒(méi)有影響。此外，腹腔注射100 nmol/kg H-1152能顯著增加海綿體神經(jīng)刺激誘導(dǎo)的勃起反應(yīng)[4]。

參考文獻(xiàn)：
1.?Ikenoya M1, Hidaka H, Hosoya T, Suzuki M, Yamamoto N, Sasaki Y. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16.
2.?Yu M1, Chen X, Wang N, Cai S, Li N, Qiu J, Brandt CR, Kaufman PL, Liu X.
H-1152 effects on intraocular pressure and trabecular meshwork morphology of rat eyes.? J Ocul Pharmacol Ther. 2008 Aug;24(4):373-9. doi: 10.1089/jop.2008.0029.
3.?Lie M1, Grover M, Whitlon DS. Accelerated neurite growth from spiral ganglion neurons exposed to the Rho kinase inhibitor H-1152. Neuroscience. 2010 Aug 25;169(2):855-62. doi: 10.1016/j.neuroscience.2010.05.020. Epub 2010 May 15.
4.?Teixeira CE1, Ying Z, Webb RC. Proerectile effects of the Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine (H-1152) in the rat penis. J Pharmacol Exp Ther. 2005 Oct;315(1):155-62. Epub 2005 Jun 23.