Identification of a novel RAMP-independent CGRP receptor antagonist

Identification of an HIV integrase inhibitor with micromolar affinity for the CGRP receptor led to the discovery of a series of structurally novel CGRP receptor antagonists. Optimization of this series produced compound 16, a low-molecular weight CGRP receptor antagonist with good pharmacokinetic pr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (22), p.6705-6708
Hauptverfasser:	Zartman, C. Blair, Bell, Ian M., Gallicchio, Steven N., Graham, Samuel L., Kane, Stefanie A., Mallee, John J., Rutledge, Ruth Z., Salvatore, Christopher A., Vacca, Joseph P., Williams, Theresa M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals antagonists binding sites Biological and medical sciences cations Cell Line CGRP Dogs HIV - enzymology HIV integrase HIV Integrase Inhibitors - chemistry HIV Integrase Inhibitors - pharmacokinetics HIV Integrase Inhibitors - pharmacology Human immunodeficiency virus Humans Hydroxypyridine Medical sciences pharmacokinetics Pharmacology. Drug treatments Protein Binding Pyridines - chemistry Pyridines - pharmacokinetics Pyridines - pharmacology RAMP-independent Rats Receptor Activity-Modifying Proteins - metabolism Receptors, Calcitonin Gene-Related Peptide - antagonists & inhibitors Receptors, Calcitonin Gene-Related Peptide - metabolism
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