Calcium-Sensing Receptor

The calcium-sensing receptor (CaSR) is a G-protein-coupled receptor (GPCR) that senses extracelluar Ca2+. The CaSR has wide tissue expression being found in the parathyroid gland, thyroid, kidney, intestine, skin, brain, heart, pancreas, bone and lung.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
6170 Cinacalcet hydrochloride
Calcium-sensing receptor (CaSR) allosteric agonist; also CYP2D2 inhibitor and Ca2+ channel blocker; orally bioavailable
4749 Strontium chloride
Calcium sensing receptor (CaSR) agonist

Antagonists

Cat No Product Name / Activity
3626 NPS 2143 hydrochloride
Selective antagonist of the calcium-sensing receptor; orally active calcilytic agent

Modulators

Cat No Product Name / Activity
6165 AC 265347
CaSR biased allosteric modulator
4387 Calhex 231 hydrochloride
Negative allosteric modulator of the calcium-sensing receptor
3815 R 568 hydrochloride
Positive allosteric modulator of the human calcium-sensing receptor

The calcium-sensing receptor (CaSR) is a G-protein-coupled receptor (GPCR) that senses extracellular Ca2+. The CaSR has wide tissue expression being found in the parathyroid gland, thyroid, kidney, intestine, skin, brain, heart, pancreas, bone and lung. First cloned from the bovine parathyroid gland in 1993, the primary role of CaSR activation is the inhibition of the release of parathyroid hormone (PTH).

CaSRs can also work independently of PTH. Local changes in extracellular Ca2+ regulate the differentiation and function of chondrocytes, osteoclasts and osteoblasts in bone function, potentially via the CaSR. It also has been implicated in the calcium absorption in the gastrointestinal system and in synaptic transmission.

The CaSR has also been implicated in numerous signal transduction pathways. Decreased binding of extracellular Ca2+ leads to conformational changes in the CaSR, initiating the phospholipase C pathway. Activation of CaSRs also inhibits adenylyl cyclase and suppresses intracellular cAMP, inhibiting cAMP-dependent pathways.

Mutations of the CaSR gene can lead to calcium related disorders such as familial hypocalciuric hypercalcemia.

External sources of pharmacological information for Calcium-Sensing Receptor :

    Literature for Calcium-Sensing Receptor

    GPCR

    GPCR Product Listing

    A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

    • Rhodopsin-like Receptors
    • Secretin-like Receptors
    • Glutamate Receptors
    • Frizzled Receptors
    • GPCR Signaling

    Calcium-Sensing Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Calcium-Sensing Receptor Human CASR NM_000388 P41180
    Mouse Casr NM_013803 Q9QY96
    Rat Casr NM_016996 P48442