Methiothepin
Based on 2 publication(s) in Google Scholar
Methiothepin (Metitepine; Ro 8-6837) is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 20229-30-5
- 分子式: C20H24N2S2
- 分子量:356.55
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Methiothepin
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生物活性
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5-HT1A Receptor |
5-HT1B Receptor |
5-HT1C Receptor |
5-HT1D Receptor |
5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT5A Receptor |
5-HT5B Receptor |
5-HT6 Receptor |
5-HT7 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Astrocyte | EC50 |
3.698 μM
Compound: 38
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Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
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[PMID: 17417631] |
| CHO | EC50 |
0.6 nM
Compound: methiothepin
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Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells
Displacement of [3H]lysergic acid from human recombinant 5HT7 receptor expressed in CHO cells
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[PMID: 16562853] |
| CHO-K1 | IC50 |
4.7 nM
Compound: Methiothepin
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Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
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[PMID: 25557493] |
| CHO-K1 | IC50 |
4.7 nM
Compound: Methiothepin
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Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
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[PMID: 25557493] |
| HEK293 | EC50 |
0.35 μM
Compound: Methiothepin
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Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay
Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay
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[PMID: 21784633] |
| HEK293 | EC50 |
0.38 nM
Compound: Metitepine
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Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
Antagonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
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[PMID: 23537943] |
| HEK293 | IC50 |
21 nM
Compound: Methiothepin
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Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of 5-CT-induced cAMP production preincubated for 15 mins followed by 5-CT addition measured after 15 mins by HTRF assay
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[PMID: 26900658] |
| HEK-293T | EC50 |
0.33 μM
Compound: Methiothepin
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Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay
Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay
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[PMID: 25052428] |
| HEK-293T | EC50 |
0.35 μM
Compound: Methiothepin
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Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay
Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay
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[PMID: 25052428] |
| HeLa | IC50 |
127 nM
Compound: methiothepin
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Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
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[PMID: 18053713] |
Methiothepin is a 5-HT receptor antagonist, with pKds of 7.10, 7.28, 7.56, and 6.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D[1]. Methiothepin mesylate also shows pKds of 7.0, 7.8, 8.74, and 8.99 for 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, respectively[2]. Methiothepin exhibits high affinity at 5-HT2A, 5HT2B, and 5HT2C with pKis of 8.50, 8.68, and 8.35, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 20229-30-5
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分子量 356.55
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分子式 C20H24N2S2
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SMILES
CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1
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別名
Metitepine; Ro 8-6837
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Insect Biochem Mol Biol
Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]2025 May:180:104312. PMID: 40245998 -
Gen Comp Endocrinol
Characterization of serotonin receptors Aj5-HTR2 and Aj5-HTR7 reveals potential roles in circadian regulation of Apostichopus japonicus. [Abstract]2026 Mar:379:114913. PMID: 41819218
純度とドキュメンテーション
参考文献
[1]. Schoeffter P, et al. 5-Hydroxytryptamine (5-HT)-induced endothelium-dependent relaxation of pig coronary arteries is mediated by 5-HT receptors similar to the 5-HT1D receptor subtype. J Pharmacol Exp Ther. 1990 Jan;252(1):387-95. [Content Brief]
[2]. Knight AR, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30. [Content Brief]
[3]. Hoyer D, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev. 1994 Jun;46(2):157-203. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Methiothepin 関連分類
HY-111491 関連分類
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