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Submit ReviewMethiothepin maleate
Discontinued Product
This product has been withdrawn from sale and is superseded by Methysergide maleate (Cat. No. 1064)
Description: 5-HT1 and 5-HT2 antagonist; also has moderate affinity for 5-ht5 and high affinity for 5-HT6 and 5-HT7
Alternative Names: Metitepine
Chemical Name: 1-[10,11-Dihydro-8-(methylthio)dibenzo(Z)[b,f]thiepin-10-yl]-4-methylpiperazine maleate
Purity: ≥99% (HPLC)
Biological Activity for Methiothepin maleate
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 for Methiothepin maleate
| M. Wt | 472.62 |
| Formula | C20H24N2S2.C4H4O4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 19728-88-2 |
| PubChem ID | 5358812 |
| InChI Key | IWDBEHWZGDSFHR-BTJKTKAUSA-N |
| Smiles | [H]OC(=O)\C=C/C(=O)O[H].CSC1=CC2=C(SC3=C(CC2N2CCN(C)CC2)C=CC=C3)C=C1 |
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.
Product Datasheets for Methiothepin maleate
References for Methiothepin maleate
References are publications that support the biological activity of the product.
Wilkinson and Middlemiss (1992) Metitepine distinguishes two receptors mediating inhibition of [3H]-5-hydroxytryptamine release in guinea pig hippocampus. Naunyn Schmiedebergs Arch.Pharmacol. 345 696 PMID: 1321958
Hoyer et al (1994) International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol.Rev. 46 157 PMID: 7938165
Wesołowska et al (2002) In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors. Pol.J.Pharmacol. 154 327 PMID: 2523486
Glenon et al (2003) Higher-end serotonin receptors: 5-HT5, 5-HT6, and 5-HT7. J.Med.Chem. 46 2795 PMID: 12825922
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Keywords: Methiothepin maleate, Methiothepin maleate supplier, moderate, affinity, 5-ht5, high, 5-ht6, 5-HT7, antagonists, 5-HT1, 5-HT2, Serotonin, 5-HT-, 5-Hydroxytryptamine, Receptors, 5-HT, Metitepine, Non-selective, 0582, Tocris Bioscience
5 Citations for Methiothepin maleate
Citations are publications that use Tocris products. Selected citations for Methiothepin maleate include:
Fisas et al (2006) Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats. Br J Pharmacol 148 973 PMID: 16783408
Meyer et al (2012) A "genome-to-lead" approach for insecticide discovery: pharmacological characterization and screening of Aedes aegypti D(1)-like DA receptors. PLoS Negl Trop Dis 6 e1478 PMID: 22292096
Newman-Tancredi et al (2001) Differential modulation by GTPgammaS of agonist and inverse agonist binding to h5-HT(1A) receptors revealed by [3H]-WAY100,635. Br J Pharmacol 132 518 PMID: 11159702
Geerts et al (1999) Involvement of 5-HT1B receptors in collar-induced hypersensitivity to 5-hydroxytryptamine of the rabbit carotid artery. Br J Pharmacol 127 1327 PMID: 10455282
Conley et al (2015) Evaluation of AaDOP2 receptor antagonists reveals antidepressants and antipsychotics as novel lead molecules for control of the yellow fever mosquito, Aedes aegypti. Oncotarget 352 53 PMID: 25332454
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.