INVESTIGADORES
TALEVI Alan
artículos
Título:
Anticonvulsant activity of artificial sweeteners: a structural link between sweettaste receptor T1R3 and brain glutamate receptors
Autor/es:
ALAN TALEVI, ANDREA V. ENRIQUE, LUIS E. BRUNO BLANCH
Revista:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Editorial:
PERGAMON-ELSEVIER SCIENCE LTD
Referencias:
Lugar: Amsterdam; Año: 2012 vol. 22 p. 472 - 474
ISSN:
0960-894X
Resumen:
A virtual screening campaign based on application of a topological discriminant function capable of identifying novel anticonvulsant agents indicated several widely-used artificial sweeteners as potential anticonvulsant candidates. Acesulfame Potassium, cyclamate and saccharin were tested in the Maximal Electroshock Seizure model (mice, ip), showing moderate anticonvulsant activity. We hypothesized a probable structural link between the receptor responsible of sweet taste and anticonvulsant molecular targets. Bioinformatic tools confirmed a highly significant sequence-similarity between taste-related protein T1R3 and several metabotropic glutamate receptors from different species, including glutamate receptors upregulated in epileptogenesis and certain types of epilepsy.
