NPS-2143 (SB262470A) hydrochloride is a potent, selective and orally active CaSR antagonist with IC50 of 43 nM.
NPS-2143 does not inhibit cytoplasmic Ca2+ responses to glutamate in HEK 293 cells engineered to express mGluRs and GABAB receptors.
NPS-2143 stimulates parathyroid hormone (PTH ) secretion from bovine parathyroid cells in vitro (EC50=39 nM) and increases plasma PTH levels in vivo.
NPS-2143 also inhibits lipopolysaccharide-induced pulmonary inflammation.
