2. Academic Validation
  3. Development of a rat parathyroid hormone 2 receptor antagonist

Development of a rat parathyroid hormone 2 receptor antagonist

  • Peptides. 2007 Apr;28(4):887-92. doi: 10.1016/j.peptides.2006.12.002.
Jonathan Kuo 1,  Ted B Usdin
Affiliations

Affiliation

  • 1 National Institute of Mental Health, Laboratory of Genetics, Building 35, Room 1B-415, Convent Drive, MSC 3728, Bethesda, MD 20892, USA. [email protected]
PMID: 17207559 DOI: 10.1016/j.peptides.2006.12.002
Abstract

The parathyroid hormone 2 (PTH2) receptor is a Family B G-protein coupled receptor most highly expressed within the brain. Current evidence suggests that tuberoinfundibular peptide of 39 residues (TIP39) is the PTH2 receptor's endogenous ligand. To facilitate investigation of the physiological function of the PTH2 receptor/TIP39 system, we have developed a novel PTH2 receptor antagonist, by changing several residues within the amino terminal domain of TIP39. Histidine(4), tyrosine(5), tryptophan(6), histidine(7)-TIP39 binds the PTH2 receptor with high affinity, has over 30-fold selectivity for the rat PTH2 receptor over the rat PTH1 receptor and displays no detectable agonist activity. This ligand should be useful for in vivo investigation of PTH2 receptor function.

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