产品
编 号:F395206
分子式:C4H7NO2
分子量:101.1
产品类型
结构图
CAS No: 57-71-6
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产品详情
生物活性:
Biacetyl monoxime (Diacetyl monoxime), a myosin ATPase inhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal muscle myosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca2+ release.
体内研究:
Biacetyl monoxime (0-200 mg/kg; i.v.; once) shows hypotensive effect.Biacetyl monoxime (0-205 mg/kg; i.p.; once) shows anticonvulsant effect against Picrotoxin (HY-101391)-induced convulsions.Animal Model:Male SHR and age-matched WKY rat
Dosage:5, 30, I00 and 200 mg/kg
Administration:Intravenous administration, 1 mL/kg, once
Result:Decreased arterial blood pressure for both strains, the SHR was significantly more responsive.
Animal Model:Male mice (20 to 25 g)
Dosage:51, 103 and 205 mg/kg in combination with intraperitoneal injection of 3.0 mg/kg Picrotoxin (HY-101391)
Administration:Intraperitoneal injection, once
Result:Showed dose-dependent anticonvulsant effect against Picrotoxin-induced convulsions.
体外研究:
Biacetyl monoxime (Diacetyl monoxime) (50 mM, 6 and 48 h) decreases cellulase secretion in C. cinerea.Biacetyl monoxime (50 mM, 2 and 4 h) disrupts the localization of the Golgi apparatus, but not that of the endoplasmic reticulum.Biacetyl monoxime (0-30 mM) induces SR Ca2+ release (no efflux inhibitors) in a concentration-dependent manner, with a maximal reduction of 72% of SR Ca2+ at pCa 6.0.Biacetyl monoxime acts as a chemical phosphatase, which has led to speculation that dephosphorylation of key Ca2+ channel proteins may be involved in its inhibition of contraction.Biacetyl monoxime does not inhibit the ATPase activity of two different myosin-I isoforms, myosin-V, or myosin-VI.Biacetyl monoxime (0-50 mM) suppresses L-type Ca2+ current of single cardiac myocytes isolated from SHR and WKY rats.Biacetyl monoxime significantly reduces the duration of both spontaneous and electrically stimulated action potentials of cultured neonatal rat cardiomyocytes.