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BL-1020, a novel antipsychotic candidate with GABA-enhancing effects: D2 receptor occupancy study in humans
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Radiology, Oncology and Radiation Science, Section of Nuclear Medicine and PET.
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2009 (English)In: European Neuropsychopharmacology, ISSN 0924-977X, E-ISSN 1873-7862, Vol. 19, no 12, 841-850 p.Article in journal (Refereed) Published
Abstract [en]

BL-1020 is a potentially novel antipsychotic, which comprises the typical antipsychotic perphenazine linked by an ester bound to gamma-aminobutyric acid (GABA), intending a simultaneous dopamine-2 (D(2)) receptor blockade and GABA facilitation in the brain. This positron emission tomography (PET) study, using [(11)C]raclopride, assessed the extent and duration of D(2) receptor occupancy (D(2) RO) and safety for single doses of BL-1020 in healthy male subjects. Overall, this study did not raise any safety concern. Single doses of 16-32 mg BL-1020 caused a dose dependent striatal D(2) RO. The 32 mg dose of BL-1020 resulted in an average D(2) RO of 44% at 4-6 h post dosing (pd), which declined to 33% at 24 h pd. Equimolar doses of BL-1020 and perphenazine resulted in similar D(2) RO at 24 h pd. Pharmacokinetic-pharmacodynamic analysis predicted that oral once daily administration of 32 mg BL-1020 would result in D(2) ROs ranging from 52 to 66% at a steady state.

Place, publisher, year, edition, pages
2009. Vol. 19, no 12, 841-850 p.
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Medical and Health Sciences
URN: urn:nbn:se:uu:diva-141412DOI: 10.1016/j.euroneuro.2009.07.009PubMedID: 19717284OAI: oai:DiVA.org:uu-141412DiVA: diva2:385564
Available from: 2011-01-11 Created: 2011-01-11 Last updated: 2015-09-24Bibliographically approved

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Appel, LieuweAntoni, Gunnar
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