Γ-Acetylenic-GABA
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IUPAC name 4-Aminohex-5-ynoic acid | |
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ECHA InfoCard | 100.165.059 |
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Properties | |
Chemical formula | C6H9NO2 |
Molar mass | 127.143 g·mol−1 |
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Hazard statements | H315, H319, H335 |
Precautionary statements | P261, P264, P264+P265, P271, P280, P302+P352, P304+P340, P305+P351+P338, P319, P321, P332+P317, P337+P317, P362+P364, P403+P233, P405, P501 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references |
Chemical compound
γ-Acetylenic GABA, also known as 4-aminohex-5-ynoic acid is a potent and irreversible inhibitor of GABA-T.[3]
Mechanism of action
Like other GABA-T inhibitors, γ-acetylenic GABA causes GABA levels in the brain to be elevated. This is due to 4-aminobutyrate transaminase being the enzyme that converts γ-aminobutyric acid to L-glutamate. Inhibiting the enzyme stops this conversion from happening.
Potential uses
Anti convulsant
Continuous administration of γ-acetylenic GABA on rats during four days was able to reduce or completely stop seizures that were induced by amygdala overstimulation.[4]
Treatment of tardive dyskinesia
A study has showed that γ-acetylenic GABA could reduce tardive dyskinesia symptoms. This result mostly happened in subjects receiving higher doses.[5]
References
- ^ https://pubchem.ncbi.nlm.nih.gov/compound/4-Aminohex-5-ynoic-acid
- ^ "4-Aminohex-5-ynoic acid". pubchem.ncbi.nlm.nih.gov.
- ^ Tell, Guy; Böhlen, Peter; Schechter, Paul J.; Koch-Weser, Jan; Agid, Yves; Bonnet, A. M.; Coquillat, Gilles; Chazot, Guy; Fischer, Catherine (February 1981). "Treatment of Huntington disease with γ ‐acetylenic GABA, an irreversible inhibitor of GABA‐ transaminase: Increased CSF GABA and homocarnosine without clinical amelioration". Neurology. 31 (2): 207. doi:10.1212/WNL.31.2.207. ISSN 0028-3878.
- ^ Myslobodsky, M. S.; Valenstein, E. S. (April 1980). "Amygdaloid kindling and the GABA system". Epilepsia. 21 (2): 163–175. doi:10.1111/j.1528-1157.1980.tb04058.x. hdl:2027.42/66112. ISSN 0013-9580. PMID 7358042.
- ^ Casey, Daniel E.; Gerlach, Jes; Magelund, Gerhard; Christensen, Torben Rosted (1980-12-01). "γ-Acetylenic GABA in Tardive Dyskinesia". Archives of General Psychiatry. 37 (12): 1376–1379. doi:10.1001/archpsyc.1980.01780250062007. ISSN 0003-990X.
- v
- t
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GATTooltip GABA transporter |
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VIAATTooltip Vesicular inhibitory amino acid transporter |
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GADTooltip Glutamate decarboxylase |
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GABA-TTooltip γ-Aminobutyrate aminotransferase |
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Antivitamin B6 |
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- See also
- Receptor/signaling modulators
- GABA receptor modulators
- GABAA receptor positive modulators
- Glutamate metabolism/transport modulators