Methiothepin maleate
Discontinued Product
Chemical Name: 1-[10,11-Dihydro-8-(methylthio)dibenzo(Z)[b,f]thiepin-10-yl]-4-methylpiperazine maleate
Purity: ≥99%
Biological Activity
5-HT2 antagonist (pKi = 8.7 - 9.2) ; also active as 5-HT1 antagonist (pKi values are 7.1 - 8.5). Also displays affinity for rodent 5-HT5B, 5-HT5A, 5-HT7 and 5-HT6 receptors (pKi values are 6.6, 7.0, 8.4 - 9.0 and 8.7 - 9.4, respectively).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Metitepine distinguishes two receptors mediating inhibition of [3H]-5-hydroxytryptamine release in guinea pig hippocampus.
Wilkinson and Middlemiss
Naunyn Schmiedebergs Arch.Pharmacol., 1992;345:696 -
International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).
Hoyer et al.
Pharmacol.Rev., 1994;46:157 -
In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors.
Wesołowska et al.
Pol.J.Pharmacol., 2002;154:327 -
Higher-end serotonin receptors: 5-HT5, 5-HT6, and 5-HT7.
Glenon et al.
J.Med.Chem., 2003;46:2795
Product Datasheets
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Citations for Methiothepin maleate
The citations listed below are publications that use Tocris products. Selected citations for Methiothepin maleate include:
5 Citations: Showing 1 - 5
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Evaluation of AaDOP2 receptor antagonists reveals antidepressants and antipsychotics as novel lead molecules for control of the yellow fever mosquito, Aedes aegypti.
Authors: Conley Et al.
Oncotarget 2015;352:53
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A "genome-to-lead" approach for insecticide discovery: pharmacological characterization and screening of Aedes aegypti D(1)-like DA receptors.
Authors: Meyer Et al.
PLoS Negl Trop Dis 2012;6:e1478
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Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats.
Authors: Fisas Et al.
Br J Pharmacol 2006;148:973
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Differential modulation by GTPgammaS of agonist and inverse agonist binding to h5-HT(1A) receptors revealed by [3H]-WAY100,635.
Authors: Newman-Tancredi Et al.
Br J Pharmacol 2001;132:518
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Involvement of 5-HT1B receptors in collar-induced hypersensitivity to 5-hydroxytryptamine of the rabbit carotid artery.
Authors: Geerts Et al.
Br J Pharmacol 1999;127:1327
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