Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging

…, CF Ferris, M Placzek, G Jones, MJ Brownstein…

Index: Fabio, Karine; Guillon, Christophe; Lacey, Carl J.; Lu, Shi-Fang; Heindel, Ned D.; Ferris, Craig F.; Placzek, Michael; Jones, Graham; Brownstein, Michael J.; Simon, Neal G. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 3 p. 1337 - 1345

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Citation Number: 9

Abstract

SRX246 is a potent, highly selective human vasopressin V1a antagonist that crosses the blood–brain barrier in rats. CNS penetration makes SRX246 an ideal candidate for potential radiolabeling and use in visualization and characterization of the role of the V1a receptor in multiple stress-related disorders. Before radiolabeling studies, cold reference analogs of SRX246 were prepared. This study describes the synthesis and in vitro screening for ...