Progress in corticotropin-releasing factor-1 antagonist development
نویسندگان
چکیده
منابع مشابه
Brain pharmacokinetics of a nonpeptidic corticotropin-releasing factor receptor antagonist.
Corticotropin-releasing factor (CRF) is known to play an important role in the body response to stress. Butyl-[2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-ethylamine (CP-154,526) is a CRF(1) antagonist showing anxiolytic activities in rats in behavioral models, suggesting that CP-154,526 crosses the blood-brain barrier. However, there is no direct evidence for this. ...
متن کاملThe potential role of a corticotropin-releasing factor receptor-1 antagonist in psychiatric disorders.
CNS Spectr 13:6 June 2008 467 NEW TREND IN PSYCHOPHARMACOLOGY The hypothalamic-pituitary-adrenal axis is a key mediator of the stress response in humans. The corticotropin-releasing factor (CRF) type 1 receptor (CRFR-1) in the pituitary gland is a gatekeeper for that response, and the CRFR-1 receptor is also present in many other moodand cognition-related neural structures. Behaviorally, a numb...
متن کاملCorticotropin-releasing Factor
Introduction Immunoreactivity similar to that of corticotropin-releasing factor (CRF) is found in regions of the central nervous system that modulate autonomic responses, including gastrointestinal functions. We examined the central nervous system effects of ovine CRF on gastric acid secretion in conscious dogs. Male beagle dogs (11-13 kg) were fitted with chronic intracerebroventricular cannul...
متن کاملCorticotropin releasing factor in neuroplasticity.
Stress is among the strongest signals promoting neuroplasticity: Stress signals, indicating real or perceived danger, lead to alterations of neuronal function and often structure, designed to adapt to the changed conditions and promote survival. Corticotropin releasing factor (CRF) is expressed and released in several types of neuronal populations that are involved in cognition, emotion and the...
متن کاملBinding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.
Corticotropin-releasing factor (CRF) receptor antagonists are under preclinical and clinical investigation for stress-related disorders. In this study the impact of receptor-ligand binding kinetics on CRF₁ receptor antagonist pharmacology was investigated by measuring the association rate constant (k₁), dissociation rate constant (k₋₁), and kinetically derived affinity at 37°C. Three aspects of...
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ژورنال
عنوان ژورنال: Drug Discovery Today
سال: 2010
ISSN: 1359-6446
DOI: 10.1016/j.drudis.2010.02.011