R. Dieden et al., IDENTIFICATION AND IN-VITRO IMMUNOSUPPRESSIVE ACTIVITY OF A SDZ-IMM-125 METABOLITE ISOLATED FROM PHENOBARBITAL-INDUCED RABBIT LIVER-MICROSOMES, Xenobiotica, 27(9), 1997, pp. 933-949
1. A metabolite of D-serine-cyclosporine A has been isolated from phen
obarbital induced rabbit liver microsomes using hplc. 2. This metaboli
te was identified by FAB, electrospray mass spectrometry as well as nm
r spectroscopy and is the result of metabolism of the vinylic methyl g
roup of the 9-carbon amino acid unique to the cyclosporins, the first
amino acid of this cyclic undecapeptide. This metabolite exhibits a si
gnificantly lower immunosuppressive activity than IMM-125 and CsA.