PCO371 is a nonpeptidyl, orally active agonist of Parathyroid hormone type 1 receptor (PTHR1). It stimulates cAMP production in COS-7 cells with an EC50 of 2.4 μmol/L. It also acts as an osteoporosis drug and significantly enhances bone mineral density (BMD) and bone strength in the lumbar vertebrae of osteopenic ovariectomized (OVX) rats. It also restores normal serum calcium levels without increasing urinary calcium in hypocalcemic thyroparathyroidectomized (TPTX) rats.