Stereoselective propranolol metabolism in two drug induced rat hepatic microsomes
Li, Zeng
Abstract
Li, Zeng
Abstract
;BNFgroup:R(+)34+3,S(-)39±7;PB group:R(+)38±17,S(-)36±10.2.Vmax.Control group:R(+)1.5+0.2,S(-)2.9±0.3;BNF group:R(+)3.8±0.3,S(-)3.3±0.5;PB group:R(+)0.07±0.03,S(-)1.94±0.07.3.Clint.Control group:R(+)60±3,S(-)170±30;BNF group:R(+)111.0±1,S(-)84± 5;PBgroup:R(+)2.0±2,S(-)56.0±1.Theenzyme.parameters compared with unpaired ttests showed that no stereoselectivity wasobserved in enzymatic affinity of threemicrosomes to enantiomers and their catalyticabilities were quite different and hadstereoselectivities.Compared with the control,microsome induced by BNF enhanced enzymeactivity to propranolol R(+)-enantiomer,andmicrosome induced by PB showed less enzymeactivity to propranolol S(-)-enantiomer whichremains the same stereoselectivities as that ofthe control.CONCLUSION Enzyme activity center
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;BNFgroup:R(+)34+3,S(-)39±7;PB group:R(+)38±17,S(-)36±10.2.Vmax.Control group:R(+)1.5+0.2,S(-)2.9±0.3;BNF group:R(+)3.8±0.3,S(-)3.3±0.5;PB group:R(+)0.07±0.03,S(-)1.94±0.07.3.Clint.Control group:R(+)60±3,S(-)170±30;BNF group:R(+)111.0±1,S(-)84± 5;PBgroup:R(+)2.0±2,S(-)56.0±1.Theenzyme.parameters compared with unpaired ttests showed that no stereoselectivity wasobserved in enzymatic affinity of threemicrosomes to enantiomers and their catalyticabilities were quite different and hadstereoselectivities.Compared with the control,microsome induced by BNF enhanced enzymeactivity to propranolol R(+)-enantiomer,andmicrosome induced by PB showed less enzymeactivity to propranolol S(-)-enantiomer whichremains the same stereoselectivities as that ofthe control.CONCLUSION Enzyme activity center
Key concepts: Stereoselectivity, Propranolol, Enantiomer, Microsome, Chemistry, Enzyme, Stereochemistry, Metabolism