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Cat. No.: HY-111491

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Methiothepin

(Synonyms: Metitepine; Ro 8-6837)

2 Cited Publications

고객리뷰

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).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 20229-30-5
화학식: C₂₀H₂₄N₂S₂
분자량:356.55

보관:

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
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
순도&문서
References
Calculators
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Bioz

Biological Activity

제품 설명

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
분자량 356.55
화학식 C₂₀H₂₄N₂S₂
SMILES

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

Metitepine; Ro 8-6837
선적

Room temperature in continental US; may vary elsewhere.
보관

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

Publications (2)

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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

순도&문서

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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

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Methiothepin

2 Cited Publications

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Publications (2)
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Methiothepin

Publications Citing Use of MedChemExpress (MCE) Methiothepin

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Publications (2)

순도&문서

References

Calculators

Help & FAQs

Methiothepin Related Classifications

HY-111491 Related Classifications