PT  - JOURNAL ARTICLE
AU  - Renê Oliveira Beleboni
AU  - Renato Guizzo
AU  - Andréia Cristina Karklin Fontana
AU  - Andrea Baldocchi Pizzo
AU  - Ruither Oliveira Gomes Carolino
AU  - Leonardo Gobbo-Neto
AU  - Norberto Peporine Lopes
AU  - Joaquim Coutinho-Netto
AU  - Wagner Ferreira dos Santos
TI  - Neurochemical Characterization of a Neuroprotective Compound from <em>Parawixia bistriata</em> Spider Venom That Inhibits Synaptosomal Uptake of GABA and Glycine
AID  - 10.1124/mol.105.017319
DP  - 2006 Jun 01
TA  - Molecular Pharmacology
PG  - 1998--2006
VI  - 69
IP  - 6
4099  - http://molpharm.aspetjournals.org/content/69/6/1998.short
4100  - http://molpharm.aspetjournals.org/content/69/6/1998.full
SO  - Mol Pharmacol2006 Jun 01; 69
AB  - The major contribution of this work is the isolation of a neuroprotective compound referred to as 2-amino-5-ureidopentanamide (FrPbAII) (Mr = 174) from Parawixia bistriata spider venom and an investigation of its mode of action. FrPbAII inhibits synaptosomal GABA uptake in a dose-dependent manner and probably does not act on Na+, K+, and Ca2+ channels, GABAB receptors, or γ-aminobutyrate:α-ketoglutarate aminotransferase enzyme; therefore, it is not directly dependent on these structures for its action. Direct increase of GABA release and reverse transport are also ruled out as mechanisms of FrPbAII activities as well as unspecific actions on pore membrane formation. Moreover, FrPbAII is selective for GABA and glycine transporters, having slight or no effect on monoamines or glutamate transporters. According to our experimental glaucoma data in rat retina, FrPbAII is able to cross the blood-retina barrier and promote effective protection of retinal layers submitted to ischemic conditions. These studies are of relevance by providing a better understanding of neurochemical mechanisms involved in brain function and for possible development of new neuropharmacological and therapeutic tools.