Bioorganic and Medicinal Chemistry Letters p. 6582 - 6585 (2011)
Update date:2022-08-05
Topics:
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.
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.
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