Uptake in brain and neurophysiological activity of two lipid esters of γ-aminobutyric acid
| Autor: | Gary W. Hesse, Victor E. Shashoua, James N. Jacob |
|---|---|
| Rok vydání: | 1988 |
| Předmět: |
Male
Central nervous system Action Potentials Hippocampus In Vitro Techniques Pharmacology Biology Aminobutyric acid Cellular and Molecular Neuroscience chemistry.chemical_compound medicine Animals Picrotoxin Neurotransmitter Triglycerides gamma-Aminobutyric Acid Brain uptake Rats Inbred Strains Population spike Prodrug In vitro Rats medicine.anatomical_structure nervous system Biochemistry chemistry |
| Zdroj: | Neuropharmacology. 27:637-640 |
| ISSN: | 0028-3908 |
| DOI: | 10.1016/0028-3908(88)90186-4 |
| Popis: | Two lipid esters of γ-aminobutyric acid (GABA), 1-linolenoyl-2,3-bis(4-aminobutyryl) propane-1,2,3-triol and 1,2-dilinolenoyl-3-(4-aminobutyryl)propane-1,2,3-triol, were found to have brain uptake indices of greater than 30% using the single-pass carotid artery injection technique. Both compounds produced dose-dependent inhibition of the evoked population spike in slices of rat hippocampus maintained in vitro . This effect was blocked reversibly by plcrotoxin. The magnitude of the inhibition produced by the lipid esters of GABA was comparable to that of similar doses of GABA, but for both compounds the duration of the effect was at least 10 times longer than that produced by GABA. These data are consistent with the idea that the lipid esters of GABA can effectively penetrate the blood-brain barrier and act as prodrugs for the delivery of GABA to the central nervous system. |
| Databáze: | OpenAIRE |
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