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Phaclofen: a GABAB blocker reduces long-duration inhibition in the neocortex

1988; Elsevier BV; Volume: 148; Issue: 3 Linguagem: Inglês

10.1016/0014-2999(88)90136-7

1879-0712

Göril Karlsson, Mario F. Pozza, Hans-Rudolf Olpe,

Ion channel regulation and function

Phaclofen, a phosphonic acid analog of baclofen, is a selective, low-affinity (high μM), GABAB receptor antagonist. As one of the first antagonists for this site, phaclofen has been employed extensively for defining the physiological and pharmacological characteristics of this receptor system. In particular, it has been used widely for examining the electrophysiological properties of GABAB receptors and for in vitro studies. Its use as a research tool has diminished somewhat with the advent of higher affinity GABAB receptor antagonists, such as CGP 55845 and related phosphinic acid derivatives.