1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

Methiothepin mesylate (Synonyms: Metitepine mesylate; Ro 8-6837 mesylate)

Cat. No.: HY-107836
Handling Instructions

Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, and also acts as an antagonist at 5-HT1, 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, with pKds of 7.10, 7.28, 7.56, 6.99, 7.0, 7.8, 8.74, and 8.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D, 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7 and pKis of 8.50, 8.68, and 8.35 for 5HT2A, 5HT2B, 5HT2C.

For research use only. We do not sell to patients.
Methiothepin mesylate Chemical Structure

Methiothepin mesylate Chemical Structure

CAS No. : 74611-28-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
10 mg USD 60 In-stock
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, and also acts as an antagonist at 5-HT1, 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7, with pKds of 7.10, 7.28, 7.56, 6.99, 7.0, 7.8, 8.74, and 8.99 for 5-HT1A, 5HT1B, 5HT1C, 5HT1D, 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7 and pKis of 8.50, 8.68, and 8.35 for 5HT2A, 5HT2B, 5HT2C.

IC50 & Target

pKd: 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D)[1], 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), 8.99 (5-HT7)[3]
pKi: 8.50 (5-HT2A), 8.68 (5-HT2B), 8.35 (5-HT2C)[2]

In Vitro

Methiothepin mesylate 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].

References
Molecular Weight

452.65

Formula

C₂₁H₂₈N₂O₃S₃

CAS No.

74611-28-2

SMILES

CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(SC)C=C24)CC1.CS(=O)(O)=O

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 125 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Methiothepin mesylate
Cat. No.:
HY-107836
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