1345249-31-1Relevant articles and documents
Discovery of a novel potent GABAB receptor agonist
Xu, Feng,Peng, Ge,Phan, Thu,Dilip, Usha,Chen, Jian Lu,Chernov-Rogan, Tania,Zhang, Xuexiang,Grindstaff, Kent,Annamalai, Thamil,Koller, Kerry,Gallop, Mark A.,Wustrow, David J.
, p. 6582 - 6585 (2011/12/04)
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 GABAB 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.