TY - JOUR
T1 - Nonpeptide corticotropin releasing hormone type 1 receptor antagonists as medications and imaging agents
AU - Contoreggi, Carlo
AU - Ayala, Alejandro
AU - Grant, Steven
AU - Eckelman, William
AU - Webster, Elizabeth
AU - Rice, Kenner
PY - 2002/11/1
Y1 - 2002/11/1
N2 - Corticotropin-releasing hormone (CRH) is produced in the brain and in the periphery and coordinates the body's response to stress. When CRH is synthesized and released from the hypothalamus, it activates the release of adrenocorticotropic hormone from the pituitary, which stimulates adrenal release of cortisol, the principal adrenal steroid hormone in primates. CRH and CRH-like molecules are produced in the CNS and act as peptide neurotransmitters. The regional actions of CRH in the CNS are varied and only partially understood. In addition to regulation of the hypothalamic-pituitary-adrenal axis, CRH coordinates other hormones as well as autonomic, immune and behavioral responses to stress. Aberrant CRH action is implicated in many diseases including addiction, depression, anxiety and eating disorders. In order to understand the physiological role of CRH and the pharmacological actions of the CRHR1 antagonists, we have developed a radiolabeled CRHR1 ligand as an in vivo imaging agent.
AB - Corticotropin-releasing hormone (CRH) is produced in the brain and in the periphery and coordinates the body's response to stress. When CRH is synthesized and released from the hypothalamus, it activates the release of adrenocorticotropic hormone from the pituitary, which stimulates adrenal release of cortisol, the principal adrenal steroid hormone in primates. CRH and CRH-like molecules are produced in the CNS and act as peptide neurotransmitters. The regional actions of CRH in the CNS are varied and only partially understood. In addition to regulation of the hypothalamic-pituitary-adrenal axis, CRH coordinates other hormones as well as autonomic, immune and behavioral responses to stress. Aberrant CRH action is implicated in many diseases including addiction, depression, anxiety and eating disorders. In order to understand the physiological role of CRH and the pharmacological actions of the CRHR1 antagonists, we have developed a radiolabeled CRHR1 ligand as an in vivo imaging agent.
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U2 - 10.1358/dof.2002.027.11.857018
DO - 10.1358/dof.2002.027.11.857018
M3 - Review article
AN - SCOPUS:0036878411
VL - 27
SP - 1093
EP - 1100
JO - Drugs of the Future
JF - Drugs of the Future
SN - 0377-8282
IS - 11
ER -