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

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 dis...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2012-02, Vol.20 (3), p.1337-1345
Hauptverfasser:	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.
Format:	Artikel
Sprache:	eng
Schlagworte:	antagonists Antidiuretic Hormone Receptor Antagonists Arginine vasopressin Arginine Vasopressin - metabolism Azetidines - chemical synthesis Azetidines - pharmacology Biological and medical sciences blood-brain barrier Blood-Brain Barrier - metabolism Cell Line chemistry Humans image analysis Ligands Medical sciences permeability PET Pharmacology. Drug treatments Positron-Emission Tomography - methods Protein Binding Radioisotopes - chemistry Radioisotopes - pharmacology Radiolabeling rats Receptors, Vasopressin - analysis screening SPECT tin Tomography, Emission-Computed, Single-Photon - methods vasopressin Vasopressin V1a antagonist
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