Calcitonin and related receptors are a family of G-protein-coupled receptors that comprises eight subtypes; CT, AMY 1, AMY 2, AMY 3, CALCR, CGRP, AM 1 and AM 2. The main function of CT receptors is to inhibit bone reabsorption and enhance calcium excretion by the kidneys.
Calcitonin and related receptors are a family of G-protein-coupled receptors that comprises eight subtypes; CT, AMY 1, AMY 2, AMY 3, CALCR, CGRP, AM 1 and AM 2. The receptors have a wide biological distribution; high concentrations are found in the brain, lung, liver, heart and spleen with lower expression levels present in the testes, gastrointestinal tract and thyroid.
The main function of CT receptors is to inhibit bone reabsorption and enhance calcium excretion by the kidneys. AMY receptors are heterodimers of the CT receptor and receptor activating modifying proteins (RAMP) 1-3, which have been implicated in type II diabetes pathology. The CALCRL receptor alone is non-functioning, but forms heterodimers with RAMPs to form the CGRP (CALCRL with RAMP1), AM 1 (CALCRL with RAMP2) and AM 2 (CALCRL with RAMP3) receptors. Their main function is inducing vasodilation, which causes hypotension. The CGRP receptor has also recently been implicated in the pathogenesis of migraine.
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
CT and CALCRL form heterodimers with RAMP1-3, forming additional calcitonin related receptors; AMY 1, AMY 2, AMY 3, CGRP, AM 1 and AM 2. (AMY 1 = CT + RAMP1, AMY 2 = CT + RAMP2, AMY 3 = CT + RAMP3, CGRP = CALCRL + RAMP1, AM 1 = CALCRL + RAMP2, AM 2 = CALCRL + RAMP3)