Voltar
Artigo Revisado por pares
BIBTEX RIS

Synthesis and biological evaluation of conformationally restricted gabapentin analogues

1999; Elsevier BV; Volume: 9; Issue: 16 Linguagem: Inglês

10.1016/s0960-894x(99)00383-2

ISSN

1464-3405

Autores

Jean‐Marie Receveur, Justin S. Bryans, Mark J. Field, Lakhbir Singh, David C. Horwell,

Tópico(s)

Cancer Treatment and Pharmacology

Resumo

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.

Referência(s)