Tag: 327.8296

Effect of hydrochloride fasudil on IL-1尾, TNF-伪 and RHO kinase in serum of patients with cerebral infarction was written by Li, Tong;Tian, Hong-ying;Deng, Yan;Su, Da-jing;He, Ning-yu. And the article was included in Hainan Yixueyuan Xuebao in 2011.Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

Objective: To explore effect of hydrochloride fasudil on IL-1尾, TNF-伪 and RHO kinase in serum of patients with cerebral infarction. Methods: A total of 186 cases with cerebral infarction were divided into two groups. Patients in observation group were treated by routine therapy and hydrochloride fasudil; while patients in control group were treated by routine therapy. Expressions of IL-1尾, TNF-伪 and RHO kinase were detected before and after treatment. The efficacy and changes of IL-1尾, TNF-伪 and RHO kinase in serum were observed and compared. Results: The efficacy was higher in the observation group than in the control group. The expressions of IL-1尾, TNF-伪 and RHO kinase were significantly decreased after treatment. But the decrease of IL-1尾, TNF-伪 and RHO kinase was more significant in the observation group than in the control group. Conclusions: Hydrochloride fasudil can improve the efficacy, inhibit the expressions of IL-1尾, TNF-伪 and RHO kinase, and protect the cerebral cells in patients with cerebral infarction. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline is a catabolite of tryptophan, the basic structure of some antihypertensive drugs, such as the peripheral vasodilators prazosin and doxazosin. The discovery of chloroquine, the most well-known drug containing this stent, has helped bring about decades of malaria control and treatment.Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Design, synthesis and biological evaluations of a long-acting, hypoxia-activated prodrug of fasudil, a ROCK inhibitor, to reduce its systemic side-effects was written by Al-Hilal, Taslim A.;Hossain, Mohammad Anwar;Alobaida, Ahmad;Alam, Farzana;Keshavarz, Ali;Nozik-Grayck, Eva;Stenmark, Kurt R.;German, Nadezhda A.;Ahsan, Fakhrul. And the article was included in Journal of Controlled Release in 2021.Electric Literature of C14H18ClN3O2S This article mentions the following:

ROCK, one of the downstream regulators of Rho, controls actomyosin cytoskeleton organization, stress fiber formation, smooth muscle contraction, and cell migration. ROCK plays an important role in the pathologies of cerebral and coronary vasospasm, hypertension, cancer, and arteriosclerosis. Pharmacol.-induced systemic inhibition of ROCK affects both the pathol. and physiol. functions of Rho-kinase, resulting in hypotension, increased heart rate, decreased lymphocyte count, and eventually cardiovascular collapse. To overcome the adverse effects of systemic ROCK inhibition, we developed a bioreductive prodrug of a ROCK inhibitor, fasudil, that functions selectively under hypoxic conditions. By masking fasudil鈥瞫 active site with a bioreductive 4-nitrobenzyl group, we synthesized a prodrug of fasudil that is inactive in normoxia. Reduction of the protecting group initiated by hypoxia reveals an electron-donating substituent that leads to fragmentation of the parent mol. Under normoxia the fasudil prodrug displayed significantly reduced activity against ROCK compared to its parent compound, but under severe hypoxia the prodrug was highly effective in suppressing ROCK activity. Under hypoxia the prodrug elicited an antiproliferative effect on disease-afflicted pulmonary arterial smooth muscle cells and pulmonary arterial endothelial cells. The prodrug displayed a long plasma half-life, remained inactive in the blood, and produced no drop in systemic blood pressure when compared with fasudil-treated controls. Due to its selective nature, our hypoxia-activated fasudil prodrug could be used to treat diseases where tissue-hypoxia or hypoxic cells are the pathol. basis of the disease. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Electric Literature of C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Although isoquinoline derivatives can be synthesized by several methods, relatively few direct methods deliver the unsubstituted isoquinoline. The Pomeranz鈥揊ritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Electric Literature of C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Efficacy and safety of fasudil in prevention of radial artery spasm during cardiac interventional diagnosis and treatment was written by Zhou, Jing;Gao, Feng;Du, Ri-ying;Bai, Huai-sheng;Li, Xiao-li. And the article was included in Zhongguo Laonianxue Zazhi in 2013.Reference of 105628-07-7 This article mentions the following:

Objective: To observe clin. efficacy of fasudil in prevention of radial artery spasm during cardiac interventional diagnosis and treatment. Methods: 481 cases of hospitalized patients with transradial coronary artery interventional diagnosis and treatment were treated by intrathecal injection of the corresponding drugs for prevention of radial artery spasm. Group I was treated with fasudil 5 mg, groupII was treated with nitroglycerin 200渭g, group III was treated with verapamil 1 mg, and observe whether radial artery spasm occurred and blood pressure, ECG changes, observe whether the local and systemic complications occurred. Results: During transradial intervention treatment, application of fasudil can more effectively prevent the occurrence of radial artery spasm, and has small effect on heart rate, blood pressure and ECG, low incidence of systemic symptoms, and local symptoms. Conclusion: fasudil hydrochloride in cardiac interventional diagnosis and treatment is safe and effective for prevention of radial artery spasm. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Reference of 105628-07-7).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. The isoquinoline structure occurs in a considerable number of alkaloids in widely separated plant families. Most traditional methods of generating isoquinoline do so via oxidative aromatization of dihydro- or tetrahydro-isoquinolines, usually offering some environmental or economic advantage.Reference of 105628-07-7

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Determination of related substances in fasudil hydrochloride by HPLC was written by Ge, Xin;Meng, Xiangjun;Li, Naran. And the article was included in Guangpu Shiyanshi in 2011.Computed Properties of C14H18ClN3O2S This article mentions the following:

The determination of related substances in fasudil hydrochloride was investigated by HPLC on C₁₈ column, with methanol-ammonium dihydrogen phosphate (30:70, adjusting pH to 3.5 卤 0.05 with phosphoric acid) as mobile phase at the detection wavelength of 275 nm. The detection limit was 0.3 mg/mL for fasudil hydrochloride, and the main compound peak could entirely sep. from related substances. The method is simple, accurate and sensitive, that can be applied for determination of related substances in fasudil hydrochloride. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Computed Properties of C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline and isoquinoline skeletons are among the most attractive frameworks with a wide range of biological and pharmacological activities. Lewis acid activation and nucleophilic attack can produce multiple regioisomers in quinolines and pyridines; isoquinolines generally only undergo attack at the 1-position.Computed Properties of C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Clinical Investigation of Fasudil for the Prevention of Cerebral Vasospasm in Extracranial Carotid Artery Stenting was written by Liu, Juan;Yao, Guo-en;Zhou, Hua-dong;Jiang, Xiao-jiang;Xie, Peng. And the article was included in Cell Biochemistry and Biophysics in 2014.Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

To evaluate fasudil hydrochloride for the prevention of cerebral vasospasm (CVS) in extra-cranial carotid angioplasty and stenting (CAS). We retrospectively analyzed 178 patients with unilateral CAS who were given i.v. fasudil hydrochloride during the perioperative period. CVS, hypotension, stroke, and mortality incidence rates were recorded. Of the cohort studied, 80.9 % patients exhibited no local CVS, asymptomatic vasospasm was observed in 17.4 % patients and symptomatic vasospasm in 1.7 % patients via DSA imaging. All CVS was relieved and symptoms disappeared after intra-arterial infusion of papaverine hydrochloride. Intracerebral hemorrhage occurred in two cases during the perioperative period, one of which resulted in death. CVS is a severe complication of CAS. Fasudil hydrochloride can rapidly relieve cerebral vasospasm, has no selective effect on cerebral vasculature, and little influence on blood pressure. It is suitable for the prevention of CVS during interventional treatment of ischemic cerebrovascular disease. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline is a catabolite of tryptophan, the basic structure of some antihypertensive drugs, such as the peripheral vasodilators prazosin and doxazosin. Most traditional methods of generating isoquinoline do so via oxidative aromatization of dihydro- or tetrahydro-isoquinolines, usually offering some environmental or economic advantage.Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Fasudil hydrochloride hydrate, a Rho-kinase inhibitor, suppresses high glucose-induced proliferation and collagen synthesis in rat cardiac fibroblasts was written by Zhou, Hong;Zhang, Kai-Xia;Li, Yong-Jun;Guo, Bing-Yan;Wang, Mei;Wang, Mian. And the article was included in Clinical and Experimental Pharmacology and Physiology in 2011.Electric Literature of C14H18ClN3O2S This article mentions the following:

Hyperglycemia promotes the proliferation of cardiac fibroblasts (CFs) and collagen synthesis in CFs. The objectives of the present study were to determine the effects of fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, on high glucose (HG)-induced proliferation of CFs and collagen production in rat CFs and to investigate the mol. mechanism of action of fasudil. Rat CFs were cultured in Dulbecco’s modified Eagle’s medium, supplemented with 5.5 or 25 mmol/L D-glucose or 5.5 mmol/L D-glucose + 19.5 mmol/L mannose, in the presence of absence of fasudil (50 or 100 渭mol/L). Proliferation was measured by the 3-(4,5-dimethyl-2 thiazoyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, whereas the production of type I collagen was evaluated using ELISA and the expression of ROCK1, c-Jun N-terminal kinase (JNK) and type I procollagen mRNA was determined by reverse transcription-polymerase chain reaction. Intracellular type I procollagen protein levels were evaluated using immunocytochem. Western blot anal. was used to evaluate the phosphorylation of myosin phosphatase target subunit 1 (MYPT1), JNK and Smad2/3, as well as c-jun protein levels. Both concentrations of fasudil effectively inhibited HG (25 mmol/L D-glucose)-induced increases in the proliferation of CFs and collagen synthesis, concomitant with suppression of HG-induced upregulation of ROCK1 and JNK mRNA expression and c-jun protein levels, as well as the phosphorylation of MYPT1, JNK and Smad2/3. These data suggest that ROCK activation is essential for the proliferation of CFs and collagen synthesis induced by HG. Fasudil suppressed HG-induced increases in the proliferation of CFs and collagen synthesis, which may be associated with inhibition of the JNK and transforming growth factor 尾/Smad pathways. The results of the present study indicate that inhibition of ROCK may be a novel therapeutic target for the prevention of diabetic cardiac fibrosis. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Electric Literature of C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Isoquinoline is a structural isomer of quinoline, which have antiseptic, antipyretic and anti-cyclic properties, and can be used as antimalarial drugs and for the preparation of other antimalarial medicine. Other industrial applications include their use as corrosion inhibitors, preservatives, and as solvents for resins and terpenes.Electric Literature of C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats was written by Qi, Lei;Lv, Tian;Cheng, Yusheng;Yu, Min;Han, Honghao;Kong, Hui;Xie, Weiping;Wang, Hong;Zhang, Yihua;Huang, Zhangjian. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Synthetic Route of C14H18ClN3O2S This article mentions the following:

Given the therapeutic efficacy of fasudil hydrochloride (F) and dichloroacetate (DCA) on pulmonary arterial hypertension (PAH), a new salt fasudil dichloroacetate (FDCA) was designed, synthesized and biol. evaluated. FDCA exhibited comparable ROCK II inhibitory activity relative to fasudil hydrochloride, and suppressed the expression of TNF-伪 and IL-6 in both PDGF-BB and hypoxia-treated pulmonary arterial smooth muscle cells (PASMCs) and endothelial cells (PAECs). Significantly, FDCA lowered mean pulmonary artery pressure (mPAP) and right ventricular systolic pressure (RVSP), and decreased right ventricular hypertrophy (RVH) in monocrotaline (MCT)-induced PAH rats. Meanwhile, FDCA remarkably decreased pulmonary artery medial thickness (PAMT) and hyperplasia, restoring the elasticity of elastic fiber, reduced cardiac hypertrophy, and attenuated fibrosis of heart and lung. Collectively, FDCA exhibited triple activities of pulmonary vasodilation, vascular remodeling inhibition and RVH inhibition, suggesting that it may be a promising agent for PAH intervention. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Synthetic Route of C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Isoquinoline is a structural isomer of quinoline, which have antiseptic, antipyretic and anti-cyclic properties, and can be used as antimalarial drugs and for the preparation of other antimalarial medicine. The Pomeranz鈥揊ritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Synthetic Route of C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Clinical Investigation of Fasudil for the Prevention of Cerebral Vasospasm in Extracranial Carotid Artery Stenting was written by Liu, Juan;Yao, Guo-en;Zhou, Hua-dong;Jiang, Xiao-jiang;Xie, Peng. And the article was included in Cell Biochemistry and Biophysics in 2014.Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

To evaluate fasudil hydrochloride for the prevention of cerebral vasospasm (CVS) in extra-cranial carotid angioplasty and stenting (CAS). We retrospectively analyzed 178 patients with unilateral CAS who were given i.v. fasudil hydrochloride during the perioperative period. CVS, hypotension, stroke, and mortality incidence rates were recorded. Of the cohort studied, 80.9 % patients exhibited no local CVS, asymptomatic vasospasm was observed in 17.4 % patients and symptomatic vasospasm in 1.7 % patients via DSA imaging. All CVS was relieved and symptoms disappeared after intra-arterial infusion of papaverine hydrochloride. Intracerebral hemorrhage occurred in two cases during the perioperative period, one of which resulted in death. CVS is a severe complication of CAS. Fasudil hydrochloride can rapidly relieve cerebral vasospasm, has no selective effect on cerebral vasculature, and little influence on blood pressure. It is suitable for the prevention of CVS during interventional treatment of ischemic cerebrovascular disease. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline is a catabolite of tryptophan, the basic structure of some antihypertensive drugs, such as the peripheral vasodilators prazosin and doxazosin. Most traditional methods of generating isoquinoline do so via oxidative aromatization of dihydro- or tetrahydro-isoquinolines, usually offering some environmental or economic advantage.Name: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats was written by Qi, Lei;Lv, Tian;Cheng, Yusheng;Yu, Min;Han, Honghao;Kong, Hui;Xie, Weiping;Wang, Hong;Zhang, Yihua;Huang, Zhangjian. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Synthetic Route of C14H18ClN3O2S This article mentions the following:

Given the therapeutic efficacy of fasudil hydrochloride (F) and dichloroacetate (DCA) on pulmonary arterial hypertension (PAH), a new salt fasudil dichloroacetate (FDCA) was designed, synthesized and biol. evaluated. FDCA exhibited comparable ROCK II inhibitory activity relative to fasudil hydrochloride, and suppressed the expression of TNF-α and IL-6 in both PDGF-BB and hypoxia-treated pulmonary arterial smooth muscle cells (PASMCs) and endothelial cells (PAECs). Significantly, FDCA lowered mean pulmonary artery pressure (mPAP) and right ventricular systolic pressure (RVSP), and decreased right ventricular hypertrophy (RVH) in monocrotaline (MCT)-induced PAH rats. Meanwhile, FDCA remarkably decreased pulmonary artery medial thickness (PAMT) and hyperplasia, restoring the elasticity of elastic fiber, reduced cardiac hypertrophy, and attenuated fibrosis of heart and lung. Collectively, FDCA exhibited triple activities of pulmonary vasodilation, vascular remodeling inhibition and RVH inhibition, suggesting that it may be a promising agent for PAH intervention. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Synthetic Route of C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Isoquinoline is a structural isomer of quinoline, which have antiseptic, antipyretic and anti-cyclic properties, and can be used as antimalarial drugs and for the preparation of other antimalarial medicine. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Synthetic Route of C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Fasudil hydrochloride hydrate, a Rho-kinase inhibitor, suppresses high glucose-induced proliferation and collagen synthesis in rat cardiac fibroblasts was written by Zhou, Hong;Zhang, Kai-Xia;Li, Yong-Jun;Guo, Bing-Yan;Wang, Mei;Wang, Mian. And the article was included in Clinical and Experimental Pharmacology and Physiology in 2011.Electric Literature of C14H18ClN3O2S This article mentions the following:

Hyperglycemia promotes the proliferation of cardiac fibroblasts (CFs) and collagen synthesis in CFs. The objectives of the present study were to determine the effects of fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, on high glucose (HG)-induced proliferation of CFs and collagen production in rat CFs and to investigate the mol. mechanism of action of fasudil. Rat CFs were cultured in Dulbecco’s modified Eagle’s medium, supplemented with 5.5 or 25 mmol/L D-glucose or 5.5 mmol/L D-glucose + 19.5 mmol/L mannose, in the presence of absence of fasudil (50 or 100 μmol/L). Proliferation was measured by the 3-(4,5-dimethyl-2 thiazoyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, whereas the production of type I collagen was evaluated using ELISA and the expression of ROCK1, c-Jun N-terminal kinase (JNK) and type I procollagen mRNA was determined by reverse transcription-polymerase chain reaction. Intracellular type I procollagen protein levels were evaluated using immunocytochem. Western blot anal. was used to evaluate the phosphorylation of myosin phosphatase target subunit 1 (MYPT1), JNK and Smad2/3, as well as c-jun protein levels. Both concentrations of fasudil effectively inhibited HG (25 mmol/L D-glucose)-induced increases in the proliferation of CFs and collagen synthesis, concomitant with suppression of HG-induced upregulation of ROCK1 and JNK mRNA expression and c-jun protein levels, as well as the phosphorylation of MYPT1, JNK and Smad2/3. These data suggest that ROCK activation is essential for the proliferation of CFs and collagen synthesis induced by HG. Fasudil suppressed HG-induced increases in the proliferation of CFs and collagen synthesis, which may be associated with inhibition of the JNK and transforming growth factor β/Smad pathways. The results of the present study indicate that inhibition of ROCK may be a novel therapeutic target for the prevention of diabetic cardiac fibrosis. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Electric Literature of C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Isoquinoline is a structural isomer of quinoline, which have antiseptic, antipyretic and anti-cyclic properties, and can be used as antimalarial drugs and for the preparation of other antimalarial medicine. Other industrial applications include their use as corrosion inhibitors, preservatives, and as solvents for resins and terpenes.Electric Literature of C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem