Bioorganic and Medicinal Chemistry Letters p. 2329 - 2334 (1999)
Update date:2022-08-03
Topics:
Receveur, Jean-Marie
Bryans, Justin S.
Field, Mark J.
Singh, Lakhbir
Horwell, David C.
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.
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