GABAB receptor agonism as a novel therapeutic modality in the treatment of gastroesophageal reflux disease.
作者： Anders Lehmann , Jörgen M. Jensen , Guy E. Boeckxstaens
DOI: 10.1016/S1054-3589(10)58012-8
关键词:
摘要: Defined pharmacologically by its insensitivity to the GABA(A) antagonist bicuculline and sensitivity GABA analogue baclofen, G protein-linked gamma-aminobutyric acid type B (GABA(B)) receptor couples adenylyl cyclase, voltage-gated calcium channels, inwardly-rectifying potassium channels. On basis of a wealth preclinical data in conjunction with early clinical observations that baclofen improves symptoms gastroesophageal reflux disease (GERD), GABA(B) has been proposed as therapeutic target for number diseases including GERD. Subsequently, there significant effort develop peripherally-restricted agonist is devoid central nervous system side effects are observed baclofen. In this article we review vitro vivo pharmacology agonists development lesogaberan (AZD3355, (R)-(3-amino-2-fluoropropyl) phosphinic acid), potent predominately window superior
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