Identification and in vitro immunosuppressive activity of a SDZ-IMM-125 metabolite isolated from phenobarbital-induced rabbit liver microsomes

1. A metabolite of D-serine-cyclosporine A has been isolated from phenobarbital induced rabbit liver microsomes using hplc. 2. This metabolite was identified by FAB, electrospray mass spectrometry as well as nmr spectroscopy and is the result of metabolism of the vinylic methyl group of the 9- carbo...

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Veröffentlicht in:	Xenobiotica 1997, Vol.27 (9), p.933-949
Hauptverfasser:	DIEDEN, R., VERBEECK, R. K., MATON, N., LATINNE, D., LHOEST, G. J. J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Chromatography, High Pressure Liquid Cyclosporins - metabolism Cyclosporins - pharmacology Immunomodulators Immunosuppressive Agents - chemistry Immunosuppressive Agents - metabolism Immunosuppressive Agents - pharmacology Magnetic Resonance Spectroscopy Male Medical sciences Microsomes, Liver - drug effects Microsomes, Liver - metabolism Pharmacology. Drug treatments Phenobarbital - pharmacology Rabbits Spectrometry, Mass, Fast Atom Bombardment
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Zusammenfassung:	1. A metabolite of D-serine-cyclosporine A has been isolated from phenobarbital induced rabbit liver microsomes using hplc. 2. This metabolite was identified by FAB, electrospray mass spectrometry as well as nmr spectroscopy and is the result of metabolism of the vinylic methyl group of the 9- carbon amino acid unique to the cyclosporins, the first amino acid of this cyclic undecapeptide. This metabolite exhibits a significantly lower immunosuppressive activity than IMM-125 and CsA.
ISSN:	0049-8254 1366-5928
DOI:	10.1080/004982597240109