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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2067992 | PMC |
| http://dx.doi.org/10.1016/j.bmc.2006.12.031 | DOI Listing |
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