Calcitonin and Related Receptors

Calcitonin and related receptors are a family of G-protein-coupled receptors that comprises eight subtypes; CT, AMY₁, AMY₂, AMY₃, CALCR, CGRP, AM₁ and AM₂. The main function of CT receptors is to inhibit bone reabsorption and enhance calcium excretion by the kidneys.

Products

Background

Literature (3)

Gene Data

Agonists
Cat. No.	Product Name / Activity
3418	Amylin
	Endogenous peptide agonist for amylin, calcitonin, CGRP and adrenomedullin receptors
6030	Amylin (rat)
	Potent endogenous peptide agonist for amylin, calcitonin, CGRP and adrenomedullin receptors
6031	Calcitonin (human)
	Endogenous calcitonin agonist; inhibits bone resorption
1159	Calcitonin (salmon)
	Affects bone formation and resorption
3012	α-CGRP (human)
	CGRP agonist
1161	CGRP (rat)
	Potent vasodilator
3555	CRSP-1
	Endogenous central calcitonin agonist
2080	PHM 27 (human)
	Potent calcitonin agonist; endogenous analog of human VIP
5031	Pramlintide
	Synthetic version of amylin (Cat. No. 3418)
2550	SUN-B 8155
	Non-peptide calcitonin agonist
Antagonists
Cat. No.	Product Name / Activity
3419	AC 187
	Potent and selective amylin antagonist
6550	AC 253
	Amylin (AMY₃) antagonist
4561	BIBN 4096
	Potent and selective CGRP antagonist
6549	cAC 253
	Amylin (AMY₃) antagonist; brain penetrant
1181	CGRP 8-37 (human)
	CGRP antagonist
1169	CGRP 8-37 (rat)
	CGRP antagonist
4314	SB 268262
	Selective non-peptide CGRP antagonist

Calcitonin and related receptors are a family of G-protein-coupled receptors that comprises eight subtypes; CT, AMY₁, AMY₂, AMY₃, CALCR, CGRP, AM₁ and AM₂. 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), AM₁ (CALCRL with RAMP2) and AM₂ (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.

External sources of pharmacological information for Calcitonin and Related Receptors :

IUPHAR Receptor Code

BJP Guide

Literature for Calcitonin and Related Receptors

Tocris offers the following scientific literature for Calcitonin and Related Receptors to showcase our products. We invite you to request* or download your copy today!

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