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CD Guillon, GA Koppel, MJ Brownstein, MO Chaney, and et a (2007)
Azetidinones as vasopressin V1a antagonists
Bioorg Med Chem 15 (5):2054-2080.
The azetidinone LY307174 (1) was identified as a screening lead for the vasopressin V1a receptor (IC50 45 nM at the human V1a receptor) based on molecular similarity to ketoconazole (2), a known antagonist of the luteinizing hormone releasing hormone receptor. Structure-activity relationships for the series were explored to optimize receptor affinity and pharmacokinetic properties, resulting in compounds with Ki values <1nM and brain levels after oral dosing approximately 100-fold higher than receptor affinities.