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Titolo:
INTESTINAL TRANSPORT AND METABOLISM OF ANALGESIC DIPEPTIDE, KYOTORPHIN - RATE-LIMITING FACTOR IN INTESTINAL-ABSORPTION OF PEPTIDE AS DRUG
Autore:
MIZUMA T; KOYANAGI A; AWAZU S;
Indirizzi:
TOKYO UNIV PHARM & LIFE SCI,SCH PHARM,DEPT BIOPHARMACEUT,1432-1 HORINOUCHI HACHIOJI TOKYO 19203 JAPAN TOKYO UNIV PHARM & LIFE SCI,SCH PHARM,DEPT BIOPHARMACEUT HACHIOJI TOKYO 19203 JAPAN
Titolo Testata:
Biochimica et biophysica acta (G). General subjects
fascicolo: 1-2, volume: 1335, anno: 1997,
pagine: 111 - 119
SICI:
0304-4165(1997)1335:1-2<111:ITAMOA>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
BRAIN; AMINOPEPTIDASE; BESTATIN; RABBIT; ARG;
Keywords:
KYOTORPHIN; INTESTINAL ABSORPTION; PEPTIDE ABSORPTION; METABOLISM; TRANSPORT; KINETIC ANALYSIS; (RAT INTESTINE);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
16
Recensione:
Indirizzi per estratti:
Citazione:
T. Mizuma et al., "INTESTINAL TRANSPORT AND METABOLISM OF ANALGESIC DIPEPTIDE, KYOTORPHIN - RATE-LIMITING FACTOR IN INTESTINAL-ABSORPTION OF PEPTIDE AS DRUG", Biochimica et biophysica acta (G). General subjects, 1335(1-2), 1997, pp. 111-119

Abstract

Intestinal transport and metabolism of kyotorphin (KTP) were studied in rat everted small intestine. KTP on the mucosal side was metabolized completely within 60 min, and any amounts of KTP were not detected on the serosal side. On the other hand, [D-Arg(2)]-KTP (D-KTP) was stable on the mucosal side to appear on the serosal side. However, N-t-butoxycarbonyl-KTP (Boc-KTP), which was metabolized on the mucosal side faster than KTP, appeared on the serosal side. In intestinal homogenate, KTP was metabolized, and the metabolic clearance (CLmet) was decreased by peptidase inhibitors, bestatin, o-phenanthrolin and tryptophan hydroxamate, In the presence of these peptidase inhibitors, the absorption clearance (CLabs) of KTP was increased. The less the CLmet of KTP was, the more the CLabs of KTP was. Meanwhile, Boc-KTP in intestinal homogenate was stable even in the absence of peptidase inhibitors. The CLabs of Boc-KTP was constant irrespective of the stability on the mucosal side. Kinetic analysis by the metabolic inhibition model indicated that the stabilization of KTP in the intestinal tissue could increase the CLabs up to 0.247 mu l/min per cm, which was as much as the CLabs of stable D-KTP. These results led to the conclusion that rate-limiting process in intestinal absorption of KTP is metabolic degradation in intestinal tissue during the absorption.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/09/20 alle ore 18:21:44