Occupancy of human brain GABAA receptors by the novel α5 subtype-selective benzodiazepine site inverse agonist α5IA as measured using [11C]flumazenil PET imaging

Author:

Eng W.,Atack J.R.,Bergstrom M.,Sanabria S.,Appel L.,Dawson G.R.,Sciberras D.,Hargreaves R.J.,Langstrom B.,Burns H.D.

Publisher

Elsevier BV

Subject

Cellular and Molecular Neuroscience,Pharmacology

Reference34 articles.

1. Preclinical and clinical pharmacology of the GABAA receptor α5 subtype-selective inverse agonist α5IA;Atack;Pharmacol. Ther.,2010

2. L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for α5-containing GABAA receptors;Atack;Neuropharmacology,2006

3. TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for α2- and α3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates;Atack;J. Pharmacol. Exp. Ther.,2006

4. The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, α5IA, is similar in rats and primates;Atack;Br. J. Pharmacol.,2009

5. Atack, J.R., Hallett, D., Tye, S., Wafford, K.A., Ryan, C., Sanabria-Bohórquez, S.M., Eng, W., Gibson, R.E., Burns, H.D., Dawson, G.R., Carling, R.W., Street, L.J., Pike, A., De Lepeleire, I., Van Laere, K., Bormans, G., de Hoon, J.N., Van Hecken, A., McKernan, R.M., Murphy, M.G., Hargreaves, R.J. Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective agonist. J. Psychopharmacol., in press-a.

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