An antagonist of 5-HT6 (Ki = 2.3 nM for the human recombinant receptor); selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM

MS 245 (oxalate) – 1 mg

Brand:
Cayman
CAS:
275363-58-1
Storage:
-20
UN-No:
Non-Hazardous - /

MS 245 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 2.3 nM for the human recombinant receptor).{42927} It is selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM, respectively), as well as 5-HT1A, 5-HT1B, 5-HT1E, 5-HT3, and 5-HT7 receptors (Kis = 720, 9,200, 4,220, 2,390, and 600 nM, respectively). MS 245 decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM). It potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (–)-nicotine (Item No. 20887) drug discrimination in rats when administered at a dose of 5 mg/kg.{42928,42929}  

 

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Description

An antagonist of 5-HT6 (Ki = 2.3 nM for the human recombinant receptor); selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM, respectively), as well as 5-HT1A, 5-HT1B, 5-HT1E, 5-HT3, and 5-HT7 receptors (Kis = 720, 9,200, 4,220, 2,390, and 600 nM, respectively); decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM); potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (–)-nicotine (Item No. 20887) drug discrimination in rats at 5 mg/kg ,,

Formal name: 5-methoxy-N,N-dimethyl-1-(phenylsulfonyl)-1H-indole-3-ethanamine, monoethanedioate

Synonyms: 

Molecular weight: 448.5

CAS: 275363-58-1

Purity: ≥98%

Formulation: A crystalline solid

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

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