41 products were found matching "K04286"!

N-acetyl Tryptamine is a structural analog of melatonin (5-methoxy-N-acetyltryptamine, Cay-14427) that binds the melatonin MT2 receptor (Ki = 41 nM). It acts as a melatonin receptor antagonist in frog skin and chicken retina and as a partial agonist in rabbit retina. N-acetyl Tryptamine is also a reaction product of...

6-hydroxy Melatonin is an active metabolite of melatonin (Cay-14427). It is formed from melatonin by the cytochrome P450 (CYP) isoform CYP1A2 in human liver microsomes. 6-hydroxy Melatonin is a melatonin 1A (MT1A), MT1B, and MT2 receptor agonist. It inhibits dopamine release from isolated rabbit retina (IC50 =...

Ramelteon is a melatonin (MT) receptor agonist (Kis = 14, 112, and 23.1 pM for human MT1, human MT2, and chick forebrain receptors, respectively). It is selective for MT1 and MT2 over MT3 receptors (Ki = 2.65 µM for hamster brain MT3 receptors) as well as a panel of benzodiazepine, dopamine, and opiate receptors,...

Agomelatine is an agonist of melatonin (MT) receptors and a derivative of melatonin (Cay-14427). It binds to MT1 and MT2 receptors (Kis = 0.14 and 0.41 nM, respectively) and has an EC50 value of 0.1 nM in a [35S]GTPgammaS binding assay using CHO cells expressing MT2 receptors. Agomelatine is also an antagonist of...

Melatonin analog, MT1/2 agonist.

Protein function: High affinity receptor for melatonin. Likely to mediates the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity. [The UniProt Consortium]

2-iodomelatonin is a potent agonist of melatonin receptor 1 (MT1, Ki = 28 pM) that is 5-fold selective for MT1 over MT2. It inhibits forskolin-stimulated cAMP production in CHO cells expressing human MT1 30-fold more potently than melatonin (Cay-14427) with an EC50 value of 11 pM. 2-iodomelatonin has been used to...

0.5 mg/ml in 1X TBS, pH7.3, with 0.5% BSA (US sourced) and 0.02% sodium azide. Additional name(s) for this target protein: MEL-1B-R, MT2, MTNR1B Protein function: High affinity receptor for melatonin. Likely to mediate the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by...

In addition to intrinsic antioxidant activities, melatonin (Cay-14427) evokes its effects through the G protein-coupled receptors MT1A (MT1) and MT1B (MT2). Luzindole is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively). Luzindole is used...

Melatonin is an indoleamine neurohormone whose levels vary in a daily cycle, thereby allowing the entrainment of the circadian rhythms of several biological functions in animals, plants, and microbes. Many biological effects of melatonin are transduced through melatonin receptors, including the MT1, MT2, and MT3...

This gene encodes one of two high affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. This gene product is an integral membrane protein that is a G-protein coupled, 7-transmembrane receptor. It is found primarily in the retina and brain although this detection requires...

8-M-PDOT is a melatonin receptor 2 (MT2) agonist (Ki = 1.12 nM). It is 5.2-fold selective for MT2 over MT1 receptors in a radioligand binding assay. Striatal microinfusion of 8-M-PDOT (10 µg/µl) increases the percentage of time spent in the open arms of the elevated plus maze, indicating anxiolytic-like activity, in...