A 7-34 analog of the parathyroid hormone-related protein has potent antagonist and partial agonist activity in vivo

Bone Miner. 1991 Mar;12(3):181-8. doi: 10.1016/0169-6009(91)90031-t.

Abstract

The biological properties of a new synthetic analog of parathyroid hormone-related protein [PTHrP-(7-34)NH2] were examined in vivo using a well characterized thyroparathyroidectomized (TPTX) rat model. The phosphaturic and urine cyclic AMP response induced by infusion of PTHrP-(1-34)NH2 (0.16 nmol/h) was inhibited by 70% (P less than 0.01, n = 6) by co-infusion of PTHrP-(7-34)NH2 at a 10-fold molar excess (1.6 nmol/h). The 7-34 PTHrP analog also antagonized the PTHrP-(1-34)NH2-induced hypercalcemia and rises in blood 1,25-dihydroxyvitamin D concentrations. However, when infused alone at a higher dose rate (8 nmol/h), PTHrP-(7-34)NH2 displayed significant PTH agonist activity. This profile contrasts to that of [Tyr-34]bPTH-(7-34)NH2 which is comparatively less potent (10-20-fold) with respect to its antagonist activity but has no appreciable agonist activity in vivo.

Publication types

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

MeSH terms

  • Animals
  • Calcitriol / blood
  • Calcium / blood
  • Cyclic AMP / urine
  • Hypercalcemia / chemically induced
  • Male
  • Parathyroid Hormone / pharmacology
  • Parathyroid Hormone-Related Protein
  • Parathyroidectomy
  • Peptide Fragments / pharmacology
  • Phosphates / urine
  • Proteins / antagonists & inhibitors*
  • Proteins / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Thyroidectomy

Substances

  • Parathyroid Hormone
  • Parathyroid Hormone-Related Protein
  • Peptide Fragments
  • Phosphates
  • Proteins
  • parathyroid hormone (7-34)amide, Tyr(34)-
  • Cyclic AMP
  • Calcitriol
  • Calcium