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Synthesis and biological evaluation of conformationally restricted Gabapentin analogues
J M Receveur1, J S Bryans, M J Field
1Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK.
Bioorganic & Medicinal Chemistry Letters
|September 7, 1999
Abstract:
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 120 nM, similar to that of Gabapentin (IC50 = 140 nM), at the Gabapentin binding site on the alpha2delta subunit of a calcium channel. Compound (3a) also reversed carrageenan induced hyperalgesia in rats.