Journal of Pharmaceutical Sciences p. 82 - 84 (1985)
Update date:2022-08-03
Topics:
Rubin
Knadler
Ho
Bechtol
Wolen
The concentrations of the (R)- and (S)-enantiomers of fenoprofen (α-methyl-3-phenoxy-benzeneacetic acid) were measured in plasma and urine of volunteers after oral administration of the (R,S)-racemate. In addition, urinary concentrations of the (R)- and (S)-4'-hydroxy metabolite of fenoprofen, the major metabolite, were measured. The (R)-enantiomer of fenoprofen was stereoselectively inverted to (S)-fenoprofen, which was the major isomeric form found in plasma and urine. A potency comparison of the enantiomers in vitro showed the (S)-isomer to be 35 times more active than the (R)-isomer in inhibiting the fatty acid cyclo-oxygenase pathway from human platelets. In vivo, the similar pharmacological potency of the two enantiomers previously observed in experimental animals may have been due to the rapid inversion of the (R)- to (S)-isomer.
View MoreAnhui Dexinjia Biopharm Co., Ltd
Contact:+86-531-82375818
Address:9 Hexie Road, kaifaqu, Taihe
Xinji City Taida Sinopec Co., Ltd.
Contact:0086-311-85341278
Address:No.6, Nanhua Road,Xinji City Road,Hebei Province,China
Contact:+33-5-34012600
Address:28 ZA des Pignès
MedicalChem(Yancheng)Manuf.Co.,Ltd.
Contact:+86-515-84383366
Address:Touzeng BinHai, YanCheng City, JiangSu Province, China
Zhuhai Rundu Pharmaceutical co.,Ltd
Contact:+86-756-7630755
Address:No.6,North Airport Road,Sanzao Town,Jinwan District
Doi:10.1021/jo00434a034
(1977)Doi:10.1016/S0022-328X(00)92673-1
(1980)Doi:10.1016/S0040-4039(99)00739-X
(1999)Doi:10.1021/jacs.7b01462
(2017)Doi:10.1021/j100141a037
(1993)Doi:10.1021/jo010376a
(2001)