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Nipecotic acid
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| ECHA InfoCard | 100.007.159 |
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| Formula | C6H11NO2 |
| Molar mass | 129.159 g·mol−1 |
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Nipecotic acid is a GABA reuptake inhibitor used in scientific research.[1][2][3] It has very little to no blood–brain barrier penetration itself, but structural modifications have been made to improve this.[4][5]
See also
[edit]References
[edit]- ^ Macdonald RL (2012). Eadie MJ, Vajda FJ (eds.). Antiepileptic drugs: pharmacology and therapeutics (First ed.). [S.l.]: Springer. p. 130. ISBN 978-3-642-64244-9.
In contrast, prolonged (1 h) exposure to gabapentin enhanced the shunting effect on CAl region excitatory postsynaptic potentials induced by the GABA uptake inhibitor, nipecotic acid, which promotes GABA release.
- ^ Takahashi K, Miyoshi S, Kaneko A, Copenhagen DR (1995). "Actions of nipecotic acid and SKF89976A on GABA transporter in cone-driven horizontal cells dissociated from the catfish retina". The Japanese Journal of Physiology. 45 (3): 457–473. doi:10.2170/jjphysiol.45.457. PMID 7474528.
- ^ Wahab A, Heinemann U, Albus K (October 2009). "Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures". Epilepsy Research. 86 (2–3): 113–123. doi:10.1016/j.eplepsyres.2009.05.008. PMID 19535226. S2CID 32999271.
- ^ Shek E (1994). "Chemical delivery systems and prodrugs of anticonvulsive drugs". Advanced Drug Delivery Reviews. 14 (2–3): 227–241. doi:10.1016/0169-409X(94)90041-8.
Nipecotic acid is a potent in vitro inhibitor of neuronal and glial GABA uptake. However, because nipecotic acid does not penetrate the blood-brain barrier (BBB) it lacks any in vivo activity [23,24].
- ^ Dhanawat M, Gupta S, Mehta DK, Das R (February 2021). "Design, Synthesis and Enhanced BBB Penetration Studies of L-serine-Tethered Nipecotic Acid-Prodrug". Drug Research. 71 (2): 94–103. doi:10.1055/a-1290-0119. PMID 33241549.
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