2000Acta Scientiarum Naturalium Universitatis SunyatseniRequires access

Stereoselective propranolol metabolism in two drug induced rat hepatic microsomes

Li, Zeng

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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

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Available 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

Key concepts: Stereoselectivity, Propranolol, Enantiomer, Microsome, Chemistry, Enzyme, Stereochemistry, Metabolism

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Stereoselective propranolol metabolism in two drug induced rat hepatic microsomes — Research Paper | ScholarLens