247089-15-2Relevant academic research and scientific papers
Synthesis and biological evaluation of conformationally restricted gabapentin analogues
Receveur, Jean-Marie,Bryans, Justin S.,Field, Mark J.,Singh, Lakhbir,Horwell, David C.
, p. 2329 - 2334 (2007/10/03)
A series of conformationally restricted Gabapentin analogues has been synthesised. The pyrrolidine analogue (R)-2-Aza-spiro[4.5]decane-4-carboxylic acid hydrochloride (3a) had an IC50 of 120nM, similar to that of Gabapentin (IC50 = 140nM), at the Gabapentin binding site on the α2δ subunit of a calcium channel. Compound (3a) also reversed carrageenan induced hyperalgesia in rats.
