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Titolo:
PHARMACOKINETIC ANALYSIS AND CELLULAR-DISTRIBUTION OF THE ANTI-HIV COMPOUND SUCCINYLATED HUMAN SERUM-ALBUMIN (SUC-HSA) IN-VIVO AND IN THE ISOLATED-PERFUSED RAT-LIVER
Autore:
JANSEN RW; OLINGA P; HARMS G; MEIJER DKF;
Indirizzi:
MEDISCH SPECTRUM TWENTE,DEPT CLIN CHEM,POB 50000 7500 KA ENSCHEDE NETHERLANDS GRONINGEN STATE UNIV,CTR PHARM,DEPT PHARMACOL & THERAPEUT 9713 AW GRONINGEN NETHERLANDS GRONINGEN STATE UNIV,DEPT PATHOL 9713 AW GRONINGEN NETHERLANDS
Titolo Testata:
Pharmaceutical research
fascicolo: 11, volume: 10, anno: 1993,
pagine: 1611 - 1614
SICI:
0724-8741(1993)10:11<1611:PAACOT>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
DEXTRAN SULFATE; INVITRO; THERAPY; REPLICATION; INFECTION; AIDS;
Keywords:
SUCCINYLATED HUMAN SERUM ALBUMIN; ANTI-HIV COMPOUND; PHARMACOKINETICS; PERFUSED RAT LIVER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
19
Recensione:
Indirizzi per estratti:
Citazione:
R.W. Jansen et al., "PHARMACOKINETIC ANALYSIS AND CELLULAR-DISTRIBUTION OF THE ANTI-HIV COMPOUND SUCCINYLATED HUMAN SERUM-ALBUMIN (SUC-HSA) IN-VIVO AND IN THE ISOLATED-PERFUSED RAT-LIVER", Pharmaceutical research, 10(11), 1993, pp. 1611-1614

Abstract

After intravenous injection of a low dose (25 mug/kg) in rats, the anti HIV-1 compound succinylated human serum albumin (Suc-HSA) is taken up mainly in the liver and spleen and is proteolytically degraded. Tenminutes after injection of I-125-Suc-HSA, 72 and 14% of the dose werefound in the liver and spleen, respectively. With immunohistochemistry we demonstrated that in both organs, Suc-HSA was specifically endocytosed in endothelial cells. In the isolated perfused rat liver preparation, liver uptake was shown to be saturable, with a K(m) of 2.9 10(-8) M and a V(max) of 2.4 mug/min/100 g body weight. The apparent K(m) and V(max) in vivo were 2.2 10(-7) M and 10.3 mug/min/100 g, respectively. Uptake in liver and spleen was inhibited by preadministration of an excess of formaldehyde-treated albumin and with polyinosinic acid, indicating the involvement of the scavenger receptor, as anticipated for such polyanionic compounds. Suc-HSA is not absorbed intact from the colon and the ileum. After injecting (i.v.) rats with a high dose of Suc-HSA (10 mg/kg), the elimination t1/2 was 3 hr, and therefore, sustained plasma levels above the concentration needed for in vitro anti-HIV-1 activity can be achieved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/08/20 alle ore 22:48:08