Inhibitors of vesicular glutamate transporter: Research advances / 国际药学研究杂志

ABSTRACT

Vesicular glutamate transporter (VGLUT), located on the vesicular membrane, is a highly specific marker of glut- amatergic neurons. VGLUT selectively transports glutamate in the cytoplasm into vesicles. VGLUT1, VGLUT2 and VGLUT3 are three subtypes of VGLUT. The VGLUT can influence the glutamatergic synaptic transmission through mediating sequestration, storage and release of glutamate. The number and activity of VGLUT can change the level of glutamate in synapse cleft through mediating sequestration, storage and release of glutamate, then influence the glutamatergic synaptic transmission. To improve this pathological situation and maintain glutamate at the physiologically relevant concentration, VGLUT inhibition is required. Several classes of competitive VGLUT inhibitors have emerged including azo dyes, substituted quinolines, fatty acids and alkaloids. This article provides a brief review on the structure and function of these potential VGLUT inhibitors.