|
Befiradol (F-13,640; NLX-112) is a very potent and highly selective 5-HT1A receptor full agonist. It has powerful analgesic and antiallodynic effects comparable to those of high doses of opioid painkillers, but with fewer and less prominent side effects, as well as little or no development of tolerance with repeated use.〔(Bernard Vacher, Bernard Bonnaud, Wouter Koek. Pyridin-2-yl-methylamine derivatives, method of preparing and application as medicine. US Patent 6020345, May 21, 1999. )〕 A SAR study revealed that replacement of the dihalophenyl moiety by 3-benzothienyl increases maximal efficacy from 84% to 124% (Ki=2.7 nM). Befiradol was discovered and developed by Pierre Fabre Médicament, a French pharmaceuticals company. In September 2013, befiradol was out-licensed to Neurolixis, a California-based biotechnology company. Neurolixis announced that it intends to re-purpose befiradol for the treatment of Levodopa-induced dyskinesia in Parkinson's disease.〔http://neurolixis.com/images/stories/nlx_pf_license_23sept13.pdf〕 In 2015, preclinical data was published describing the activity of befiradol in animal models of Parkinson's disease.〔http://www.sciencedirect.com/science/article/pii/S001448861530008X〕 == See also == * Eptapirone * Flesinoxan * F-15,599 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Befiradol」の詳細全文を読む スポンサード リンク
|