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Cat. No.: HY-111491

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Methiothepin

(Synonyms: Metitepine; Ro 8-6837)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Methiothepin (Metitepine; Ro 8-6837) is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

For research use only. We do not sell to patients.

CAS No.: 20229-30-5
Formula: C₂₀H₂₄N₂S₂
Molecular Weight:356.55

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Methiothepin Chemical Structure

CAS No.: 20229-30-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

5-HT_1A Receptor

5-HT_1B Receptor

5-HT_1C Receptor

5-HT_1D Receptor

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

5-HT_5A Receptor

5-HT_5B Receptor

5-HT₆ Receptor

5-HT₇ Receptor

All 5-HT Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Astrocyte	EC₅₀	3.698 μM Compound: 38	Antiproliferative activity against mouse astrocyte cells by MTT assay Antiproliferative activity against mouse astrocyte cells by MTT assay	[PMID: 17417631]
CHO	EC₅₀	0.6 nM Compound: methiothepin	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	[PMID: 16562853]
CHO-K1	IC₅₀	4.7 nM Compound: Methiothepin	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	[PMID: 25557493]
CHO-K1	IC₅₀	4.7 nM Compound: Methiothepin	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	[PMID: 25557493]
HEK293	EC₅₀	0.35 μM Compound: Methiothepin	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	[PMID: 21784633]
HEK293	EC₅₀	0.38 nM Compound: Metitepine	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	[PMID: 23537943]
HEK293	IC₅₀	21 nM Compound: Methiothepin	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	[PMID: 26900658]
HEK-293T	EC₅₀	0.33 μM Compound: Methiothepin	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	[PMID: 25052428]
HEK-293T	EC₅₀	0.35 μM Compound: Methiothepin	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	[PMID: 25052428]
HeLa	IC₅₀	127 nM Compound: methiothepin	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	[PMID: 18053713]

In Vitro

Methiothepin is a 5-HT receptor antagonist, with pK_ds of 7.10, 7.28, 7.56, and 6.99 for 5-HT_1A, 5HT_1B, 5HT_1C, 5HT_1D^[1]. Methiothepin mesylate also shows pK_ds of 7.0, 7.8, 8.74, and 8.99 for 5-HT_5A, 5-HT_5B, 5-HT₆, and 5-HT₇, respectively^[2]. Methiothepin exhibits high affinity at 5-HT_2A, 5HT_2B, and 5HT_2C with pK_is 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.

Chemical Information

CAS No. 20229-30-5
Molecular Weight 356.55
Formula C₂₀H₂₄N₂S₂
SMILES

CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1
Synonyms

Metitepine; Ro 8-6837
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

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Journal Impact Factor

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

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (2)
Purity & Documentation
References

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Methiothepin

Publications Citing Use of MedChemExpress (MCE) Methiothepin

All 5-HT Receptor Isoforms