Phaclofen Explained

Phaclofen, or phosphonobaclofen, is a selective antagonist for the GABA_B receptor.^[1] It was the first selective GABA_B antagonist discovered, but its utility was limited by the fact that it does not cross the blood brain barrier.^[2]

Notes and References

1. Phaclofen: a peripheral and central baclofen antagonist . Kerrn D, Ong J, Prager R, Gynther B, Curtis D . Brain Research . 405 . 3 March 1987 . 1 . 150–154 . 10.1016/0006-8993(87)90999-1. 3032346 . 29595421 .
2. J Med Chem . Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists . 7650685 . August 18, 1995 . 10.1021/jm00017a016 . Froestl W, Mickel SJ, von Sprecher G, Diel PJ, Hall RG, Maier L, Strub D, Melillo V, Baumann PA, Bernasconi R, et. al. . 38 . 17 . 3313–3331 .