Methiothepin maleate (Synonyms: Metitepine) |
| Catalog No.GC17360 |
5-HT antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 19728-88-2
Sample solution is provided at 25 µL, 10mM.
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Methiothepin is a non-selective antagonist of the serotonin (5-HT) receptor.[1] It is a potent antagonist of 5-HT1A and 5-HT1B (IC50 = 16 nM and Ki = 0.2 nM, respectively) as well as 5-HT2A, 5-HT2B, and 5-HT2C receptors (Kis = 3.16, 2.08, and 4.46 nM, respectively).[2],[3],[4] Methiothepin binds to 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7 receptors with Kd values of 100, 15.8, 1.8, and 1 nM, respectively.1 It has been used to characterize the role of serotonin in various biological processes, including renal vasodilation and gastrointestinal function.[5],[6]
Reference:
[1]. Hoyer, D., Clarke, D.E., Fozard, J.R., et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol. Rev. 46(2), 157-203 (1994).
[2]. Lovenberg, T.W., Baron, B.M., de Lecea, L., et al. A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms. Neuron 11(3), 449-458 (1993).
[3]. Hamblin, M.W., Metcalf, M.A., McGuffin, R.W., et al. Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: A homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity. Biochem. Bioph. Res. Commun. 184(2), 752-759 (1992).
[4]. Knight, A.R., Misra, A., Quirk, K., et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT2A, 5-HT2B and 5-HT2C receptors. Naunyn Schmiedebergs Arch. Pharmacol. 370(2), 114-123 (2004).
[5]. García-Pedraza, J.Á., García, M., Martín, M.L., et al. Pharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats. Clin. Exp. Pharmacol. Physiol. 42(6), 640-647 (2015).
[6]. Varanasi, S., Chi, J., and Stephens, R.L., Jr. Methiothepin attenuates gastric secretion and motility effects of vagal stimulants at the dorsal vagal complex. Eur. J. Pharmacol. 436(1-2), 67-73 (2002).
| Cas No. | 19728-88-2 | SDF | |
| Synonymes | Metitepine | ||
| Chemical Name | (R)-1-methyl-4-(8-(methylthio)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine maleate | ||
| Canonical SMILES | CN1CCN(CC1)[C@@H](C2=C3)CC4=CC=CC=C4SC2=CC=C3SC.OC(/C=C\C(O)=O)=O | ||
| Formula | C20H24N2S2.C4H4O4 | M.Wt | 472.62 |
| Solubility | 0.5mg/mL in ethanol, 30mg/mL in DMSO, or in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1159 mL | 10.5793 mL | 21.1586 mL |
| 5 mM | 423.2 μL | 2.1159 mL | 4.2317 mL |
| 10 mM | 211.6 μL | 1.0579 mL | 2.1159 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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