A non-selective 5-HT receptor antagonist; potent antagonist of 5-HT1A and 5-HT1B (IC50 = 16 nM and Ki = 0.2 nM

Methiothepin (maleate) – 100 mg

Brand:
Cayman
CAS:
19728-88-2
Storage:
-20
UN-No:
Non-Hazardous - /

Methiothepin is a non-selective antagonist of the serotonin (5-HT) receptor.{39327} 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).{40435,40434,41063} 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.{39327} It has been used to characterize the role of serotonin in various biological processes, including renal vasodilation and gastrointestinal function.{40402,40436}  

 

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Description

A non-selective 5-HT receptor antagonist; potent antagonist of 5-HT1A and 5-HT1B (IC50 = 16 nM and Ki = 0.2 nM, respectively); potent antagonist of 5-HT2A, 5-HT2B, and 5-HT2C receptors (Kis = 3.16, 2.08, and 4.46 nM, respectively); binds to 5-HT5A, 5-HT5B, 5-HT6, and 5-HT7 receptors (Kds = 100, 15.8, 1.8, and 1 nM, respectively); has been used to characterize the role of serotonin in various biological processes

Formal name: 1-[10,11-dihydro-8-(methylthio)dibenzo[b,f]thiepin-10-yl]-4-methyl-piperazine, (2Z)-butenedioate

Synonyms:  Metitepine

Molecular weight: 472.6

CAS: 19728-88-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience

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