ALBUMIN BINDING AND BRAIN UPTAKE OF 6-FLUORO-DL-TRYPTOPHAN - COMPETITION WITH L-TRYPTOPHAN

被引：10

作者：

CHANUT, E ^{[1
]}

ZINI, R ^{[1
]}

TROUVIN, JH ^{[1
]}

RIANT, P ^{[1
]}

TILLEMENT, JP ^{[1
]}

JACQUOT, C ^{[1
]}

机构：

[1] UFR MED,PHARMACOL LAB,F-94010 CRETEIL,FRANCE

来源：

BIOCHEMICAL PHARMACOLOGY | 1992年 / 44卷 / 10期

关键词：

D O I：

10.1016/0006-2952(92)90112-V

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

We investigated potential competition between L-tryptophan (TRP) and 6-fluoro-DL-tryptophan (6-F-TRP) for binding to albumin and for passage through the blood-brain barrier (BBB). In experiments based on equilibrium dialysis, albumin (600 muM) bound about 80% of TRP and 50% of 6-F-TRP with affinity constants (K(a)) of 3.7 +/- 0.04 x 10(4) and 0.62 +/- 0.01 x 10(4) M-1, respectively. Competitive inhibition was assessed as the decrease in the apparent K(a) (K(a)') of TRP in the presence of 6-F-TRP, with no modification of the N value. Competition between TRP, 6-F-TRP and L-valine (VAL) for passage across the BBB was demonstrated using two approaches. When administered concomitantly with TRP or 6-F-TRP to rats, VAL decreased brain uptake of TRP and 6-F-TRP and reversed their action on serotonin. In Oldendorf's model, 6-F-TRP and VAL decreased the brain uptake of TRP.

引用

页码：2082 / 2085

页数：4

共 16 条

[1] EFFECTS OF ALBUMIN, AMINO-ACIDS, AND CLOFIBRATE ON THE UPTAKE OF TRYPTOPHAN BY THE RAT-BRAIN [J].