1.
Bioorg Med Chem Lett
; 21(21): 6582-5, 2011 Nov 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21920749
RESUMO
Structure-activity studies have led to a discovery of 3-(4-pyridyl)methyl ether derivative 9d that has 25- to 50-fold greater functional potency than R-baclofen at human and rodent GABA(B) receptors in vitro. Mouse hypothermia studies confirm that this compound crosses the blood-brain barrier and is approximately 50-fold more potent after systemic administration.