| Bioactivity | Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM[1][2]. | ||||||||||||
| Target | GABA Receptor | ||||||||||||
| Invitro | Nipecotic acid (1 mM) activated inward unitary currents when applied to outside-out patches of paraventricular neurones[1]. | ||||||||||||
| In Vivo | Nipecotic acid does not readily cross the blood-brain barrier (BBB)[2]. | ||||||||||||
| Name | Nipecotic acid | ||||||||||||
| CAS | 498-95-3 | ||||||||||||
| Formula | C6H11NO2 | ||||||||||||
| Molar Mass | 129.16 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Barrett-Jolley R, et, al. Nipecotic acid directly activates GABA(A)-like ion channels. Br J Pharmacol. 2001 Jul;133(5):673-8. [2]. Dhanawat M, et, al. Design, Synthesis and Enhanced BBB Penetration Studies of L-serine-Tethered Nipecotic Acid-Prodrug. Drug Res (Stuttg). 2021 Feb;71(2):94-103. |