Title : Occupancy of Dopamine D3 and D2 Receptors by Buspirone: A [11C]-(+)-PHNO PET Study in Humans.

Pub. Date : 2016 Jan

PMID : 26089182






5 Functional Relationships(s)
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1 The anxiolytic drug buspirone has been proposed as a potential strategy as findings suggest that this drug has high in vitro affinity for DRD3, binds to DRD3 in brain of living non-human primate, and also disrupts psychostimulant self-administration in preclinical models. Buspirone dopamine receptor D3 Homo sapiens
2 The anxiolytic drug buspirone has been proposed as a potential strategy as findings suggest that this drug has high in vitro affinity for DRD3, binds to DRD3 in brain of living non-human primate, and also disrupts psychostimulant self-administration in preclinical models. Buspirone dopamine receptor D3 Homo sapiens
3 No study has explored the occupancy of DRD3 by buspirone in humans. Buspirone dopamine receptor D3 Homo sapiens
4 Here, we used positron emission tomography (PET) and the D3-preferring probe, [(11)C]-(+)-PHNO, to test the hypothesis that buspirone will occupy (decreases [(11)C]-(+)-PHNO binding) the DRD3 more readily than the DRD2. Buspirone dopamine receptor D3 Homo sapiens
5 [(11)C]-(+)-PHNO binding in DRD2- and DRD3-rich areas was decreased by the highest (60-120 mg), but not the lowest (30 mg), doses of buspirone. Buspirone dopamine receptor D3 Homo sapiens