Author(s)
L.
Gilfillan, A.
Blair, B. J.
Morris, J. A.
Pratt, L.
Schweiger, S.
Pimlott, A.
Sutherland
ISBN
2040-2503
Publication year
2013
Periodical
Medchemcomm
Periodical Number
7
Volume
4
Pages
1118-1123
Author Address
Sutherland, A
Univ Glasgow, Sch Chem, WestCHEM, Joseph Black Bldg, Glasgow G12 8QQ, Lanark, Scotland
Univ Glasgow, Sch Chem, WestCHEM, Glasgow G12 8QQ, Lanark, Scotland
Univ Glasgow, Inst Neurosci & Psychol, Glasgow G12 8QQ, Lanark, Scotland
Univ Strathclyde, Strathclyde Inst Pharm & Biomed Sci, Ctr Neurosci, Glasgow G4 0RE, Lanark, Scotland
Univ Aberdeen, Sch Med & Dent, John Mallard Scottish PET Ctr, Aberdeen AB25 2ZD, Scotland
Univ Glasgow, West Scotland Radionuclide Dispensary, Glasgow G11 6NT, Lanark, Scotland
North Glasgow Univ Hosp NHS Trust, Glasgow G11 6NT, Lanark, Scotland
A focused library of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones containing sites for C-11-, F-18- and I-123-labelling have been prepared and evaluated against membrane expressing human recombinant metabotropic glutamate 2 receptor (mGluR2). The compounds were found to be non-competitive antagonists with nanomolar affinity. HPLC evaluation of the physiochemical properties of these compounds identified two candidates for PET and SPECT imaging of mGluR2.