Azetidinones as vasopressin V1a antagonists

Azetidinones as vasopressin V1a antagonists

The azetidinone LY307174 ( 1) was identified as a screening lead for the vasopressin V1a receptor (IC 50 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...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2007-03, Vol.15 (5), p.2054-2080
Hauptverfasser: Guillon, Christophe D., Koppel, Gary A., Brownstein, Michael J., Chaney, Michael O., Ferris, Craig F., Lu, Shi-fang, Fabio, Karine M., Miller, Marvin J., Heindel, Ned D., Hunden, David C., Cooper, Robin D.G., Kaldor, Stephen W., Skelton, Jeffrey J., Dressman, Bruce A., Clay, Michael P., Steinberg, Mitchell I., Bruns, Robert F., Simon, Neal G.
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Antidiuretic Hormone Receptor Antagonists
Azetidines - blood
Azetidines - pharmacokinetics
Azetidines - pharmacology
Azetidinone
Biological and medical sciences
Brain - metabolism
CHO Cells
CNS penetration
Cricetinae
Cricetulus
Dogs
Hormones. Endocrine system
Humans
Magnetic Resonance Spectroscopy
Medical sciences
Models, Molecular
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Oral bioavailability
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Rats
Spectrometry, Mass, Fast Atom Bombardment
Vasopressin
Vasopressin V1a antagonists
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Zusammenfassung:The azetidinone LY307174 ( 1) was identified as a screening lead for the vasopressin V1a receptor (IC 50 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 K i values
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2006.12.031