Methysergide (maleate)

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Cat No: 27658

Biochemicals - Receptor Pharmacology

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 recep...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

5HT 5HT1 5HT2 HT 1A HT1E 5HT1A 5HT1E 5HT1F HT1F 5HT1B HT1B 12 1F 1B 2A 5HT2A 2C 5HT2C HT2C HT2A HT2B 5HT2B 2B 1D 5HT1D HT1D GR 127935 anti-nociceptive 1257-58-5 29605-96-7 32537-90-9 52502-68-8 87387-76-6 NSC186061

Product Overview:
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.

Size	1 mg
Shipping	dry ice
CAS Number	129-49-7
Molecular Formula	C₂₁H₂₇N₃O₂ • C₄H₄O₄
SMILES	OC(/C=C\C(O)=O)=O.CN1C=C2C3=C1C=CC=C3C4=C[C@@H](C(N[C@H](CO)CC)=O)CN(C)[C@]4([H])C2
Molecular Weight	469,5
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2939.69
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.