A serotonin receptor antagonist active at 5-HT1 (pKi = 7.8 for 5-HT1B)

Metergoline – 100 mg

Brand:
Cayman
CAS:
17692-51-2
Storage:
-20
UN-No:
Non-Hazardous - /

Metergoline is a serotonin (5-HT) receptor antagonist that is active at 5-HT1 (pKi = 7.8 for 5-HT1B), 5-HT2, (pKi = 8.64, 8.75, and 8.75 for 5-HT2A, 5-HT2B, and 5-HT2C respectively), and 5-HT7 receptor subtypes.{41065,41063} It blocks 5-HT7 receptor-stimulated cAMP production (IC50 = 321 nM) in HEK293 cells.{34420} Metergoline has been widely used to study serotonin receptor function, but it also dose-dependently inhibits voltage-dependent sodium and potassium channels transfected into Xenopus oocytes.{34421,41064} Formulations containing metergoline have been studied for the treatment of hormone dysfunction, seasonal affective disorder, and anxiety.{34421}  

 

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Description

A serotonin receptor antagonist active at 5-HT1 (pKi = 7.8 for 5-HT1B), 5-HT2, (pKi = 8.64, 8.75, and 8.75 for 5-HT2A, 5-HT2B, and 5-HT2C respectively), and 5-HT7 receptors; blocks 5-HT7 receptor-stimulated cAMP production (IC50 = 321 nM); dose-dependently inhibits voltage-dependent sodium and potassium channels

Formal name: N-[[(8β)-1,6-dimethylergolin-8-yl]methyl]-carbamic acid, phenylmethyl ester

Synonyms: 

Molecular weight: 403.5

CAS: 17692-51-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Neuroendocrinology

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