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Titolo:
TISSUE DISTRIBUTION AND METABOLISM IN RAT OF AN ETHYNESULPHONAMIDE WITH FILARICIDAL ACTIVITY
Autore:
RADEMBINO N; DESSALLES MC; TROUVIN JH; LOISEAU PM; GAYRAL P; MAHUZIER G; RAPP M; LABARRE P; GODENECHE D; MADELMONT JC; MAURIZIS JC; VEYRE A; CHABARD JL;
Indirizzi:
UNIV PARIS 11,FAC PHARM,PARASITOL LAB,5 RUE JEAN BAPTISTE CLEMENT F-92296 CHATENAYMALABRY FRANCE UNIV PARIS 11,FAC PHARM,PARASITOL LAB F-92296 CHATENAYMALABRY FRANCE UNIV PARIS 11,FAC PHARM,LAB METHODOL BIOANALYT F-92296 CHATENAYMALABRY FRANCE UNIV PARIS 11,FAC PHARM,PHARMACOL LAB F-92296 CHATENAYMALABRY FRANCE INSERM,U71 CLERMONT FERRAN FRANCE FAC PHARM,CHIM ANALYT LAB CLERMONT FERRAN FRANCE
Titolo Testata:
Xenobiotica
fascicolo: 1, volume: 27, anno: 1997,
pagine: 73 - 85
SICI:
0049-8254(1997)27:1<73:TDAMIR>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
12
Recensione:
Indirizzi per estratti:
Citazione:
N. Radembino et al., "TISSUE DISTRIBUTION AND METABOLISM IN RAT OF AN ETHYNESULPHONAMIDE WITH FILARICIDAL ACTIVITY", Xenobiotica, 27(1), 1997, pp. 73-85

Abstract

1. The tissue distribution and metabolism of a new filaricidal agent P903 (N-[(2-phenylethynyl)sulfonyl]morpholine) were studied in rat. 2. After s.c. administration of C-14 and C-13 P903, the T-max in the blood was observed on day 2. Elimination was slow and > 95% was bound to protein. Radioactivity was distributed in the whole organism but particularly in erythrocytes and the lymphatic channel. Four days later, > 60% of the radioactivity was excreted in urine and faeces at equal amounts and 15% remained at the injection point. 3. In all biological fluids tested no P903 was found but only its metabolites.4. One principalmetabolite, the N-[(2-phenyloxo-2-ethane) sulphonyl] morpholine or oxosulphonamide was identified in blood, urine and faeces as compared with the reference compound by GC/MS and NMR. This latter molecule was detected following hydrolysis by hydrochloric acid but not with beta glucuronidase/sulphatase. 5. Unconjugated and conjugated oxosulphonamiderepresented > 85% of the radioactivity al all times tested in blood bur only 38 and 35% respectively of urinary and faecal radioactivity onday 1 after the administration of the labelled drug. 6. Thus, P903 israpidly converted to a reactive metabolite, probably an oxirene, which is then conjugated with endogenous components to form conjugated oxosulphonamide and an unknown metabolite. The role of this reactive metabolite in antifilarial activity seems to be very important in understanding the mechanism of action of P903.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/07/20 alle ore 22:31:23