Melatonin Receptors

Melatonin receptors are a group of high affinity Gi/G0 protein-coupled receptors, which are split into two subtypes; MT1 and MT2. They are widely distributed with high concentrations found in the brain (especially in the suprachiasmatic nucleus) and in the retina.

Products
Background
Gene Data

Agonists

Cat No Product Name / Activity
0357 N-Acetyltryptamine
Melatonin partial agonist (MT1/MT2). Also MT3 antagonist
0443 6-Chloromelatonin
Melatonin agonist
0737 2-Iodomelatonin
High affinity melatonin agonist
3550 Melatonin
Endogenous hormone; agonist at MT1 and MT2
1035 8-M-PDOT
Melatonin agonist
0680 2-Phenylmelatonin
Potent melatonin agonist

Antagonists

Cat No Product Name / Activity
1218 DH 97
MT2 receptor antagonist
0877 Luzindole
Competitive melatonin MT1/MT2 antagonist
1034 4-P-PDOT
MT2 antagonist
0623 Prazosin hydrochloride
MT3 antagonist, also α1 and α2B antagonist

Ligands

Cat No Product Name / Activity
0896 GR 135531
High affinity melatonin MT3 ligand

Melatonin receptors are a group of high affinity Gi/G0 protein-coupled receptors, which are split into two subtypes; MT1 and MT2. A third melatonin receptor, MT3, was proposed to exist but it has since been shown to be the hamster homolog of human quinone reductase 2 and is therefore not considered within this GPCR classification.

MT1 and MT2 receptors are widely distributed with high concentrations found in the brain (especially in the suprachiasmatic nucleus) and in the retina. Lower expression levels are seen in the kidney, heart, lung and liver. Melatonin receptors regulate a variety of physiological and neuroendrocrine functions including control of the endogenous circadian rhythm, thermoregulation and prolactin expression. The human genes encoding MT1 and MT2 receptors are located on chromosome 4q35.1 and chromosome 11q21-22 respectively.

External sources of pharmacological information for Melatonin Receptors :

Melatonin Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
MT1 Human MTNR1A NM_005958 P48039
Mouse Mtnr1a NM_008639 Q61184
Rat Mtnr1a XM_341441 Q9ESJ3
MT2 Human MTNR1B NM_005959 P49286
Mouse Mtnr1b NM_145712 Q8CIQ6
Rat Mtnr1b XM_345899 Q9JLR8