Calcitonin and Related Receptors

Calcitonin and related receptors are a family of G-protein-coupled receptors that comprises of 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

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 receptor agonist; inhibits bone resorption
1159	Calcitonin (salmon)
	Affects bone formation and resorption
3012	α-CGRP (human)
	CGRP receptor agonist
1161	CGRP (rat)
	Potent vasodilator
3555	CRSP-1
	Endogenous central calcitonin receptor agonist
2080	PHM 27 (human)
	Potent calcitonin receptor agonist; endogenous analog of human VIP
5031	Pramlintide
	Synthetic version of amylin (Cat. No. 3418)
2550	SUN-B 8155
	Non-peptide calcitonin (CT) receptor agonist
Antagonists
Cat No	Product Name / Activity
3419	AC 187
	Potent and selective amylin receptor antagonist
4561	BIBN 4096
	Potent and selective CGRP receptor antagonist
1181	CGRP 8-37 (human)
	CGRP₁ receptor antagonist
1169	CGRP 8-37 (rat)
	CGRP₁ receptor antagonist
4314	SB 268262
	Selective non-peptide CGRP₁ antagonist

Calcitonin and related receptors are a family of G-protein-coupled receptors that comprises of 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

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