Central nervous system effects of thyrotropin-releasing hormone and its analogues: Opportunities and perspectives for drug discovery and development

Research output: Contribution to journalReview article

29 Scopus citations

Abstract

Besides its well-known endocrine role in the thyroid system, thyrotropin-releasing hormone (L-pyroglutamyl-L-histidyl-L-prolinamide) has been long recognized as a modulatory neuropeptide. After a brief overview of the extrahypothalamic and receptor distribution, and of the neurophysiological, neuropharmacological and neurochemical effects of this tripeptide, this review discusses efforts devoted to enhance therapeutically beneficial central nervous system effects via structural modifications of the endogenous peptide. An enormous array of maladies affecting the brain and the spinal cord has been a potential target for therapeutic interventions involving agents derived from thyrotropin-releasing hormone as a molecular lead. Successful development of several centrally active analogues and recent accounts of efforts aimed at improving metabolic stability, selectivity and bioavailability are highlighted.

Original languageEnglish
Pages (from-to)133-169
Number of pages37
JournalProgress in Drug Research
Volume59
DOIs
StatePublished - 2002

Keywords

  • Analogue
  • Central nervous system
  • Drug development
  • Metabolism
  • Mimetic
  • Neurochemistry
  • Neurological diseases
  • Pharmacology
  • Prodrug
  • Receptor
  • Thyrotropin-releasing hormone

Fingerprint Dive into the research topics of 'Central nervous system effects of thyrotropin-releasing hormone and its analogues: Opportunities and perspectives for drug discovery and development'. Together they form a unique fingerprint.

  • Cite this