Effects of barbiturates on facilitative glucose transporters are pharmacologically specific and isoform selective.

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Haspel HC, Stephenson KN, Davies-Hill T, El-Barbary A, Lobo JF, Croxen RL, Mougrabi W, Koehler-Stec EM, Fenstermacher JD, Simpson IA

Effects of barbiturates on facilitative glucose transporters are pharmacologically specific and isoform selective.

J Membr Biol. 1999 May 1;169(1):45-53. doi: 10.1007/pl00005900.

PubMed ID

10227851 [ View in PubMed

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Abstract

Barbiturates inhibit GLUT-1-mediated glucose transport across the blood-brain barrier, in cultured mammalian cells, and in human erythrocytes. Barbiturates also interact directly with GLUT-1. The hypotheses that this inhibition of glucose transport is (i) selective, preferring barbiturates over halogenated hydrocarbon inhalation anesthetics, and (ii) specific, favoring some GLUT-# isoforms over others were tested. Several oxy- and thio-barbiturates inhibited [3H]-2-deoxyglucose uptake by GLUT-1 expressing murine fibroblasts with IC50s of 0.2-2.9 mm. Inhibition of GLUT-1 by barbiturates correlates with their overall lipid solubility and pharmacology, and requires hydrophobic side chains on the core barbiturate structure. In contrast, several halogenated hydrocarbons and ethanol (all 10 mm). Thus, barbiturates selectively inhibit glucose transport by some, but not all, facilitative glucose transporter isoforms.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Butabarbital	Solute carrier family 2, facilitated glucose transporter member 1	Protein	Humans	Unknown	Inhibitor	Details