Melatonin Receptors
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.
- IUPHAR Receptor code: MT1, MT2
- BJP Guide: Melatonin Receptors
Melatonin Receptors - More Information
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.
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 |
Melatonin Receptor Products
Featured Products |
|
Cat.No. |
Product Name / Activity |
| 0877 | Luzindole |
| Competitive melatonin MT1/MT2 antagonist | |
| 1034 | 4-P-PDOT |
| MT2 antagonist | |
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 antagonist | |
Other |
|
Cat.No. |
Product Name / Activity |
| 0896 | GR 135531 |
| High affinity melatonin MT3 ligand | |
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