A 5-HT1 receptor agonist and 5-HT2 receptor antagonist; binds to recombinant human 5-HT1A (KD = 23.44 nM)

Methysergide (maleate) – 1 mg

Brand:
Cayman
CAS:
129-49-7
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Methysergide is an agonist of the serotonin (5-HT) receptor subtype 5-HT1 and an antagonist of 5-HT2 receptors.{39327,47724} It binds to recombinant human 5-HT1A (KD = 23.44 nM), 5-HT1E (Ki = 229.09 nM), 5-HT1F (Ki = 33.88 nM), and rodent 5-HT1B receptors (KD = 1,513.56 nM).{47724} It also binds to recombinant human 5-HT2A (Ki = 2.69 nM) and 5-HT2C receptors (KD = 1.26 nM) and is an insurmountable antagonist at 5-HT2B receptors. It inhibits vasoconstriction induced by 5-HT (Item No. 14332) in isolated postmortem human basilar arterial spiral strips (pA2 = 8.07).{47725} Methysergide decreases external carotid blood flow in a dose-dependent manner in vagosympathectomized dogs, an effect that is inhibited by the 5-HT1B/1D receptor antagonist GR127935 (Item No. 29651).{47726} It has antinociceptive activity in mouse models of pain induced by intrathecal injection of substance P (Item No. 24035), glutamate, NMDA (Item No. 14581), AMPA (Item No. 14571), or kainic acid.{47727} Methysergide reduces zymosan-induced paw edema in rats when administered at a dose of 10 mg/kg.{47728} Formulations containing methysergide were previously used in the prevention and treatment of vascular headaches.  

 

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Description

A 5-HT1 receptor agonist and 5-HT2 receptor antagonist; binds to recombinant human 5-HT1A (KD = 23.44 nM), 5-HT1E (Ki = 229.09 nM), 5-HT1F (Ki = 33.88 nM), and rodent 5-HT1B receptors (KD = 1,513.56 nM); binds to recombinant human 5-HT2A (Ki = 2.69 nM) and 5-HT2C receptors (KD = 1.26 nM) and is an insurmountable antagonist at 5-HT2B receptors; inhibits 5-HT-induced vasoconstriction in isolated postmortem human basilar arterial spiral strips (pA2 = 8.07); decreases external carotid blood flow in a dose-dependent manner in vagosympathectomized dogs; has antinociceptive activity in mouse models of pain induced by substance P, glutamate, NMDA, AMPA, or kainic acid; reduces zymosan-induced paw edema in rats at 10 mg/kg

Formal name: 9,10-didehydro-N-[(1S)-1-(hydroxymethyl)propyl]-1,6-dimethyl-ergoline-8β-carboxamide, 2Z-butenedioate

Synonyms:  Desernil|NSC 186061

Molecular weight: 469.5

CAS: 129-49-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Immunology & Inflammation||Research Area|Neuroscience|Pain Research

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