Binds with high affinity to MT3 melatonin sites in hamster brain, and low affinity (and no efficacy) at MT1 and MT2 melatonin receptors and thus can be used to discriminate between the melatonin receptor subtypes.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 100 mM in ethanol|
Preparing Stock Solutions
The following data is based on the product molecular weight 275.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.63 mL||18.16 mL||36.32 mL|
|5 mM||0.73 mL||3.63 mL||7.26 mL|
|10 mM||0.36 mL||1.82 mL||3.63 mL|
|50 mM||0.07 mL||0.36 mL||0.73 mL|
References are publications that support the products' biological activity.
Dubocovich (1995) Melatonin receptors: are there multiple subtypes? TiPS 16 50 PMID: 7762083
Lucchelli et al (1997) Investigation into the contractile response of melatonin in the guinea-pig isolated proximal colon: the role of 5-HT4 and melatonin receptors. Br.J.Pharmacol. 121 1775 PMID: 9283717
If you know of a relevant reference for GR 135531, please let us know.
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Keywords: GR 135531, supplier, High, affinity, melatonin, MT3, ligands, Receptors, GR135531, 5MCANAT, 5-MCA-NAT, Melatonin, (MT), Receptors, Melatonin, (MT), Receptors, Tocris Bioscience
5 Citations for GR 135531
Citations are publications that use Tocris products. Selected citations for GR 135531 include:
Crooke et al (2013) Melatonin and its analog 5-methoxycarbonylamino-N-acetyltryptamine potentiate adrenergic receptor-mediated ocular hypotensive effects in rabbits: significance for combination therapy in glaucoma. J Pharmacol Exp Ther 346 138 PMID: 23591996
Kojima et al (2011) Melatonin inhibits tachykinin NK2 receptor-triggered 5-HT release from guinea pig isolated colonic mucosa. Br J Pharmacol 162 1179 PMID: 21091649
Tunstall et al (2011) MT2 receptors mediate the inhibitory effects of melatonin on nitric oxide-induced relaxation of porcine isolated coronary arteries. Br J Pharmacol 336 127 PMID: 20959363
Sjöblom et al (2001) Peripheral melatonin mediates neural stimulation of duodenal mucosal bicarbonate secretion. J Pharmacol Exp Ther 108 625 PMID: 11518737
Loma et al (2015) Diadenosine tetraphosphate induces tight junction disassembly thus increasing corneal epithelial permeability. J Neurosci 172 1045 PMID: 25297531
Do you know of a great paper that uses GR 135531 from Tocris? If so please let us know.
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