Article
Mapping the binding pocket of a novel, high-affinity, slow dissociating tachykinin NK3 receptor antagonist: biochemical and electrophysiological characterization.
Neuropharmacology - 1 Nov 2014
Malherbe Pari, Knoflach Frédéric, Marcuz Anne, Bohnert Claudia, Weber Michael, Knust Henner, Ratni Hasane, Spooren Will, Ballard Theresa M, Bissantz Caterina
Abstract excerpt
The NK3 receptor is a GPCR that is prominently expressed in limbic areas of the brain, many of which have been implicated in schizophrenia. Phase II clinical trials in schizophrenia with two selective NK3 antagonists (osanetant and talnetant) have demonstrated significant improvement in positive symptoms. The objective of this study was to characterize the properties of a novel dual NK2/NK3 antagonist, RO5328673....
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