Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists

A series of 2-aryloxy-4-alkoxy-pyridines (1) was identified as novel, selective, and orally active antagonists of the corticotropin-releasing factor 1 (CRF1) receptor. Among these, compound 2 (CP-316311) is a potent and selective CRF1 receptor antagonist with an IC50 value of 6.8 nM in receptor bind...

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Veröffentlicht in:	Journal of medicinal chemistry 2008-03, Vol.51 (5), p.1377-1384
Hauptverfasser:	Chen, Yuhpyng L, Braselton, John, Forman, James, Gallaschun, Randall J, Mansbach, Robert, Schmidt, Anne W, Seeger, Thomas F, Sprouse, Jeff S, Tingley, F. David, Winston, Elizabeth, Schulz, David W
Format:	Artikel
Sprache:	eng
Schlagworte:	Action Potentials - drug effects Administration, Oral Adrenocorticotropic Hormone - blood Animals Antidepressive Agents - chemical synthesis Antidepressive Agents - chemistry Antidepressive Agents - pharmacology Autoradiography Biological and medical sciences Brain - physiology Cell Line Corticotropin-Releasing Hormone - pharmacology Crystallography, X-Ray Hormones. Endocrine system Humans In Vitro Techniques Isomerism Male Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pituitary Gland - metabolism Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Radioligand Assay Rats Rats, Sprague-Dawley Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Reflex, Startle - drug effects Structure-Activity Relationship
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