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Phaclofen, or phosphonobaclofen, is a selective antagonist for the GABAB receptor.[1] It was the first selective GABAB antagonist discovered, but its utility was limited by the fact that it does not cross the blood brain barrier.[2]
References
^David I.B. KerrCorresponding author contact information, Jennifer Ong, Rolf H. Prager, Bruce D. Gynther, David R. Curtis (3 March 1987). "Phaclofen: a peripheral and central baclofen antagonist". Brain Research. 405 (1): 150–154. doi:10.1016/0006-8993(87)90999-1. PMID3032346. S2CID29595421. {{cite journal}}: |author= has generic name (help)CS1 maint: multiple names: authors list (link)
^Froestl W, Mickel SJ, von Sprecher G, Diel PJ, Hall RG, Maier L, Strub D, Melillo V, Baumann PA, Bernasconi R, et al. (August 18, 1995). "Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists". J Med Chem. 38 (17): 3313–3331. doi:10.1021/jm00017a016. PMID7650685.