Title of article
Synthesis and biological evaluation of conformationally restricted gabapentin analogues
Author/Authors
Jean-Marie Receveur، نويسنده , , Justin S. Bryans، نويسنده , , Mark J. Field، نويسنده , , Lakhbir Singh، نويسنده , , David C. Horwell، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1999
Pages
6
From page
2329
To page
2334
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 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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1999
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790336
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