Journal article
Neurochemical Characterization of a Neuroprotective Compound from Parawixia bistriata Spider Venom That Inhibits Synaptosomal Uptake of GABA and Glycine
Molecular pharmacology, v 69(6), pp 1998-2006
01 Jun 2006
PMID: 16551783
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
The major contribution of this work is the isolation of a neuroprotective compound referred to as 2-amino-5-ureidopentanamide (FrPbAII) (M sub(r) = 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 super(+), K super(+), and Ca super(2+) channels, GABA sub(B) receptors, or gamma -aminobutyrate: alpha -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.
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Details
- Title
- Neurochemical Characterization of a Neuroprotective Compound from Parawixia bistriata Spider Venom That Inhibits Synaptosomal Uptake of GABA and Glycine
- Creators
- Rene Beleboni - Universidade de São PauloRenato GuizzoAndreia Cristina Karklin FontanaAndrea PizzoRuither Oliveira Gomes CarolinoLeonardo Gobbo-NetoNorberto LopesJoaquim Coutinho-NettoWagner dos Santos
- Publication Details
- Molecular pharmacology, v 69(6), pp 1998-2006
- Publisher
- American Society for Pharmacology and Experimental Therapeutics (ASPET)
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000237688100028
- Scopus ID
- 2-s2.0-33745179229
- Other Identifier
- 991020099917104721
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- Collaboration types
- Domestic collaboration
- International collaboration
- Web of Science research areas
- Pharmacology & Pharmacy