1-(5-isoquinolinesulfonyl)-2-methylpiperazine

-2-メチルピペラジン

関

H-7

English Journal

• Protective effect of hydroxyfasudil, a Rho kinase inhibitor, on ventral prostatic hyperplasia in the spontaneously hypertensive rat.

• Holmström F1, Shimizu S1, Shimizu T1, Higashi Y1, Martin DT2, Honda M3, Saito M1.
• The Prostate.Prostate.2015 Nov;75(15):1774-82. doi: 10.1002/pros.23063. Epub 2015 Aug 19.
• BACKGROUND: Rho kinase (ROCK) pathway is associated with various cellular functions, such as smooth muscle contraction, inflammatory response, and cell proliferation. The spontaneously hypertensive rat (SHR) is commonly used genetically hypertensive rat model which develops hyperplastic morphologica
• PMID 26286428

• HA-1077 inhibits cell migration/invasion of oral squamous cell carcinoma.

• Moreira Carboni Sde S1, Rodrigues Lima NA, Pinheiro NM, Tavares-Murta BM, Crema VO.
• Anti-cancer drugs.Anticancer Drugs.2015 Oct;26(9):923-30. doi: 10.1097/CAD.0000000000000267.
• Oral squamous cell carcinoma (OSCC) is the most malignant lesion occurring in the head and neck. The Rho-kinases (ROCKs), effectors of Rho proteins, are involved in actin cytoskeletal organization, cell migration, and maintenance cortex. The HA-1077 inhibits the ROCKs. This study aimed to evaluate t
• PMID 26181228

• Protective effect of a novel Rho kinase inhibitor WAR-5 in experimental autoimmune encephalomyelitis by modulating inflammatory response and neurotrophic factors.

• Li YH1, Yu JZ1, Xin YL1, Feng L1, Chai Z2, Liu JC2, Zhang HZ2, Zhang GX3, Xiao BG4, Ma CG5.
• Experimental and molecular pathology.Exp Mol Pathol.2015 Oct;99(2):220-8. doi: 10.1016/j.yexmp.2015.06.016. Epub 2015 Jun 23.
• The Rho-kinase (ROCK) inhibitor Fasudil has proven beneficial in experimental autoimmune encephalomyelitis (EAE). Given the small safety window of Fasudil, we are looking for novel ROCK inhibitors, which have similar or stronger effect on EAE with greater safety. In this study, we report that WAR-5,
• PMID 26112093

Japanese Journal

• 線溶療法　　急性期脳梗塞に対する蛋白リン酸化酵素阻害剤：塩酸ファスジル（エリル）の効果―二重盲検試験の結果―:二重盲検試験の結果

• 渋谷 正人,佐藤 真一,鈴木 善男
• 脳卒中 26(4), 607-612, 2004
• … Fasudil (hexahydro-1-(5-isoquinolinesulfonyl)-1H-1, 4-diazepine hydrochloride or AT877, HA1077, Eril) is a unique vasodilating and brain protecting drug. … Thus, inhibition of these protein kinases by fasudil can explain its clinical effects.<BR>Hydroxylated metabolite of fasudil (M3) similarly inhibits both Rho and C kinases with longer biological half-life of about 5 hours compared with that of fasudil (45 min) after intravenous infusion. …
• NAID 130003631557

• Substance P Causes Adhesion of Neutrophils to Endothelial Cells via Protein Kinase C

• Tominaga Koji,Honda Kenji,Akahoshi Aya [他],MAKINO Yasuo,KAWARABAYASHI Tatsuhiko,TAKANO Yukio,KAMIYA Hiro-o
• Biological & pharmaceutical bulletin 22(11), 1242-1245, 1999-11-15
• … adhesion was inhibited by the tachykinin NK_1 receptor antagonist (+)-(2S, 3S)-3-(2-Methoxybenzylamino)-2-phenylpiperidine (CP-99,994) and also by the protein kinase C inhibitors 1-(5-Isoquinolinesulfonyl)-2-methyl piperazine (H-7) and bisindolylmaleimide (BIM), but not by the protein kinase A inhibitor N-[2-(p-Bromocinnamylamino) ethyl]-5-isoquinoline sulfonamide …
• NAID 110003639584

• 蛋白リン酸化酵素阻害剤:塩酸ファスジル(エリル〓)の創製

• 曽根 孝範
• 有機合成化学協会誌 54(9), 794-800, 1996-09-01
• … 1- (5-Isoquinolinesulfonyl) homopiperazine hydrochloride (fasudil) had more potent vasodilatory effect to vertebral artery than diltiazem. …
• NAID 10001841290