235791-25-0Relevant academic research and scientific papers
An in vitro investigation into conformational aspects of gabapentin
Bryans, Justin S.,Horwell, David C.,Ratcliffe, Giles S.,Receveur, Jean-Marie,Rubin, J. Ronald
, p. 715 - 721 (2007/10/03)
Conformational analysis of constrained cyclohexane systems was pioneered fifty years ago by Barton and Hassel. We now report an investigation based on a conformational analysis of a number of novel cyclohexane based Gabapentin analogues coupled with their in vitro evaluation at the Gabapentin binding site. These data are used to propose a possible binding conformation for Gabapentin. Copyright (C) 1999 Elsevier Science Ltd.
Synthesis and biological evaluation of conformationally restricted gabapentin analogues
Receveur, Jean-Marie,Bryans, Justin S.,Field, Mark J.,Singh, Lakhbir,Horwell, David C.
, p. 2329 - 2334 (2007/10/03)
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.
