Detail of "303-53-7"

Reference

Inhibition of liver microsomal epoxide hydrase by cyproheptadine epoxide

Inhibition of liver microsomal epoxide hydrase by cyproheptadine epoxide. Pachecka, J.; Salmona, M.; Belvedere, G.; Cantoni, L.; Mussini, E.; Garattini, S. (Ist. Ric. Farmacol. "Mario Negri", Milan, Italy). Experientia, 33(4), 484-5 (English) 1977. CODEN: EXPEAM. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 4, 7 Epoxide hydrase (EC 4.2.1.64) [51004-26-3] of rat liver microsomes was inhibited in vitro by cyproheptadine epoxide (I) [54191-04-7], stimulated by cyclobenzaprine [303-53-7] or cyclobenzaprine epoxide [58256-08-9], and unaffected by cyproheptadine [969-33-5], carbamazepine [298-46-4], or carbamazepine epoxide [36507-30-9]. The role of epoxide formation in carcinogenesis is discussed.

Activity of liver microsomal monoxygenases on some epoxide-forming tricyclic drugs

Activity of liver microsomal monoxygenases on some epoxide-forming tricyclic drugs. I. Kinetics in vitro. Pachecka, J.; Salmona, M.; Cantoni, L.; Mussini, E.; Pantarotto, C.; Frigerio, A.; Belvedere, G. (Ist. Ric. Farmacol. 'Mario Negri', Milan, Italy). Xenobiotica, 6(10), 593-8 (English) 1976. CODEN: XENOBH. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 7 Carbamazepine [298-46-4] and cyclobenzaprine [303-53-7] (0.1 to 1mM) were metabolized in vitro by liver microsomes to carbamazepine epoxide (I) [36507-30-9] and cyclobenzaprine epoxide (II) [58256-08-9] resp., with Km values 0.34 and 0. 58256-08-9 and 36507-30-9 are also in the experiment.26 mM resp. and Vmax values 0.41 and 0.99 nmole/min/mg protein resp. The in vitro formation of I was increased from 1.8 to 3.9 nmole/min/mg protein following pretreatment of rats with carbamazepine (50 mg/kg, for 7 days). SKF 525A inhibited II formation completely and that of I by 80%. .