Synthesis and biological evaluation of conformationally restricted Gabapentin analogues. |
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| Authors: | J M Receveur J S Bryans M J Field L Singh D C Horwell |
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| Institution: | Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK. |
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| Abstract: | A series of conformationally restricted Gabapentin analogues has been synthesised. The pyrrolidine analogue (R)-2-Aza-spiro4.5]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. |
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