Detail of "2976-75-2"

Reference

Nonlinear formation of propranolol metabolites in dogs after portacaval transpositions

Nonlinear formation of propranolol metabolites in dogs after portacaval transpositions. Lo, Man Wai; Pond, Susan M.; Effeney, David J.; Silber, Bernie M.; Riegelman, Sidney; Tozer, Thomas N. (Sch. Pharm., Univ. California, San Francisco, CA 94143, USA). J. Pharmacokinet. Biopharm., 12(4), 401-12 (English) 1984. CODEN: JPBPBJ. ISSN: 0090-466X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The formation of 4 major metabolites of propranolol [525-66-6] by the liver was examd. at steady state in 3 dogs that had undergone surgical portacaval transposition, following which injection of drug into the hindlimb delivers the total dose to the liver. Propranolol was infused directly into the liver via a hindlimb vein at dose rates of 1.01-6.3 mg/min. The formations of 4-hydroxypropranolol [10476-53-6], a-naphthoxylactic acid [2976-75-2], and propranolol glycol [36112-95-5] were saturable. Vmax And Km values were detd. at steady state by relating the rate of excretion of each metabolite into bile and urine to the blood concn. of propranolol. The formation of propranolol glucuronide [66322-66-5] was a 1st order process. The use of a dog with a portacaval transposition has permitted development of a method to est., in vivo, the kinetic properties of enzymes responsible for hepatic first-pass metab. of drugs.

Synthesis of some N-acyl derivatives of optically active trans-2-amino-1-cyclohexanols

Synthesis of some N-acyl derivatives of optically active trans-2-amino-1-cyclohexanols. Marona, Henryk; Pekala, Elzbieta (Department of Chemical Technology of Drugs, Collegium Medicum, Jagiellonian University, Krakow 30-688, Pol.). Acta Poloniae Pharmaceutica, 53(2), 111-115 (English) 1996 Polish Pharmaceutical Society. CODEN: APPHAX. ISSN: 0001-6837. DOCUMENT TYPE: Journal CA Section: 24 (Alicyclic Compounds) Optically active N-acyl derivs. (e.Several substances with their cas registry numbers 2976-75-2 and 94-75-7 may be metioned in this study.g. I; R1,R2 given: H,H;Me,Me) of D(+)- or L(-)-trans-2-amino-1-cyclohexanol were obtained by acylation either with the appropriate acid chloride or with free 4-N-acetylaminophenoxyacetic acid . In the case of N-acylation with acyl chlorides, D(+)- or L(-)-trans-2-amino-1-cyclohexanol hydrogen (+)-tartrates were used. These reactions were carried out in two-phase system (toluene-water) in the presence of K2CO3. .