Description: Has moderate affinity for 5-ht5 and high affinity for 5-ht6 and 5-HT7. Also antagonist at 5-HT1 and 5-HT2
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
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent 5-HT2 antagonist, also active as 5-HT1 antagonist. Differentiates 5-HT1D sub-types. Also displays affinity for rodent 5-HT5B, 5-HT5A, 5-HT7 and 5-HT6 receptors (pK1 values are 6.6, 7.0, 8.4 and 8.7 respectively).
Compound Libraries
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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 Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
47.26
100
Preparing Stock Solutions
The following data is based on the product molecular weight 472.62. 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
2.12 mL
10.58 mL
21.16 mL
5 mM
0.42 mL
2.12 mL
4.23 mL
10 mM
0.21 mL
1.06 mL
2.12 mL
50 mM
0.04 mL
0.21 mL
0.42 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
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
(1989) The peripheral actions of 5-HT. Ed. Fozard. Oxford. PMID: