Fasudil hydrochloride

Details:

Melting point     220.5°; mp 219.3° (Shirotani)
storage temp.     Inert atmosphere,Store in freezer, under -20°C
solubility     H2O: >200 mg/mL
form     solid
color     white
Water Solubility     Soluble in water and dimethyl sulfoxide. Insoluble in ethanol.
Merck     14,3942
InChIKey    LFVPBERIVUNMGV-UHFFFAOYSA-N
CAS DataBase Reference    105628-07-7(CAS DataBase Reference)
Safety Information
Risk Statements     22
Safety Statements     36-60
WGK Germany     3
RTECS     HM4031166
HS Code     29339900
Toxicity    LD50 in mice, rats (mg/kg): 67.5, 59.9 i.v.; 124.5, 123.2 s.c.; 273.9, 335.0 orally (Koga)
MSDS Information
Provider    Language
SigmaAldrich    English
Fasudil hydrochloride Usage And Synthesis
Indications and Usage    Fasudil Hydrochloride is a new drug with a wide range of pharmacological effects, developed by Asahi Kasei Corporation (Japan.) It is a cardiovascular and cerebrovascular drug which improves symptoms of ischemic cerebrovascular disease such as cerebral vasospasm following subarachnoid hemorrhage. It has significant neuroprotective and therapeutic effects for ischemic cerebrovascular disease, and is suited for clinical use, particularly at the grassroots level to reduce mortality and improve quality of life.
Mechanisms of Action    Fasudil Hydrochloride is an isoquinoline sulfonamide derivative which can relax separated cerebral blood vessels, inhibit the shrinkage of separated blood vessels caused by calcium influx, inhibit different mechanisms of brain blood vessel contraction from contractile agents, and inhibit intracellular calcium ion activity without reducing calcium ion concentration. Fasudil Hydrochloride is an RHO kinase inhibitor which dilates vessels, reduces tension of endothelial cells, and improves microcirculation of brain tissue without producing or exacerbating diversion of blood to the brain, by increasing activity of myosin light chain phosphatase. At the same time, it can protect nerves against apoptosis and promote their regeneration. Fasudil Hydrochloride promotes recovery of neural function and reduces clinical symptoms.
Adverse reactions    Adverse reactions after use can include intracranial hemorrhage, gastrointestinal bleeding, pulmonary hemorrhage, nasal bleeding, subcutaneous bleeding, and loss of consciousness, etc., as well as abnormal liver function. Low blood pressure, anemia, leukopenia, renal dysfunction, polyuria, rashes, and fever, etc. occur occasionally.
Warnings and Precautions    Patients with intracranial hemorrhage or possibility thereof, or low blood pressure, should not use. Patients with diabetes mellitus, cerebral arterial sclerosis, severe disturbance of consciousness, subarachnoid hemorrhages with cerebrovascular disorders, and liver or kidney dysfunction, or those over 70 years old, pregnant, or children should use with caution. Breastfeeding women should stop while using the drug. Fasudil Hydrochloride can only be administered via intravenous drip.
Description    Fasudil hydrochloride, a novel calcium antagonistic vasodilator, was marketed for the treatment of cerebral vasospasm following subarachnoid hemorrhage (SAH). Fasudil is also a potent inhibitor of myosin light chain kinase and protein kinase C. In contrast to other calcium channel blockers, which regulate the influx of calcium ions through the cell membrane but not involved in the intracellular regulatory mechanism of the calcium, fasudil was suggested to have an intracellular mode of action in relaxing vascular smooth muscle. In patients with neurological deficits due to vasospasm, fasudil decreased the occurrence of angiographic severe and symptomatic vasospasm and cerebral infarction without decreasing systemic blood pressure. Fasudil is reportedly in clinical trials for acute ischemic stroke, sequelae of cerebral vascular diseases and angina pectoris.
Originator    Asahi Chemical (Japan)
Uses    vasodilator, potent Rho-kinase inhibitor
Brand name    Eril