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pubmed-article:10476863pubmed:abstractTextA 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.lld:pubmed
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pubmed-article:10476863pubmed:articleTitleSynthesis and biological evaluation of conformationally restricted Gabapentin analogues.lld:pubmed
pubmed-article:10476863pubmed:affiliationParke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK.lld:pubmed
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