In vivo occupancy of D2 dopamine receptors by nafadotride

B Levant, NR Vansell - Neuropsychopharmacology, 1997 - Elsevier
Nafadotride has been proposed as a selective antagonist for the D3 dopamine receptor.
This drug has been shown to exhibit selectivity between D2 and D3 dopamine receptors in
in vitro assay systems; however, the in vivo D2/D3 selectivity of the compound has not been
determined. In this study, protection against inactivation by EEDQ was used as a measure of
in vivo occupancy of D2 receptors by behaviorally relevant doses of nafadotride (0.1–10
mg/kg, SC and IP) in adult, male Sprague-Dawley rats. Ex vivo [3H] spiperone binding was …
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