Therapeutic potential of CRF receptor antagonists: a gut-brain perspective

Expert Opin Investig Drugs. 2001 Apr;10(4):647-59. doi: 10.1517/13543784.10.4.647.

Abstract

Activation of the corticotropin-releasing factor (CRF) family of neuropeptide receptors in the brain and periphery appears to mediate stress-related changes in a variety of physiological and functional domains. Comparative pharmacology of CRF receptor agonists suggests that CRF, urocortin, sauvagine and urotensin consistently mimic, and conversely peptide CRF receptor antagonists lessen, the functional consequences of stressor exposure. Together with the development of novel non-peptide CRF receptor antagonists, a growing number of CRF receptor selective ligands are available to elucidate the neurobiology and physiological role of CRF systems. The present review considers available preclinical evidence as well as results from one Phase II clinical trial which address the hypothesis that CRF receptor antagonists may represent a new option for pharmacotherapy of stress-related disorders.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Anti-Anxiety Agents / pharmacology
  • Anti-Inflammatory Agents / pharmacology
  • Feeding and Eating Disorders / drug therapy
  • Gastrointestinal Motility / drug effects
  • Humans
  • Intestinal Diseases / drug therapy
  • Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
  • Receptors, Corticotropin-Releasing Hormone / physiology

Substances

  • Anti-Anxiety Agents
  • Anti-Inflammatory Agents
  • Receptors, Corticotropin-Releasing Hormone