Atipamezole (hydrochloride)

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Cat No: 9001181

Biochemicals - Receptor Pharmacology

Atipamezole is an antagonist of α2A-adrenergic receptors (α2A-ARs; Ki = 1.86 nM).{25705,25706} It is selective for α2A-ARs over α2B- and α1-ARs (Kis = 1,949.83 and 13,300 nM, respectively), as well as over 40 receptors, ion channels, and transporters ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole, monohydrochloride

Correlated keywords:

104054-27-5 Antisedan MPV1248 MPV-1248

Product Overview:
Atipamezole is an antagonist of α2A-adrenergic receptors (α2A-ARs; Ki = 1.86 nM).{25705,25706} It is selective for α2A-ARs over α2B- and α1-ARs (Kis = 1,949.83 and 13,300 nM, respectively), as well as over 40 receptors, ion channels, and transporters (IC50s = 540->10,000 nM). Atipamezole (0.04, 0.08, and 1.2 mg/kg) reverses bradycardia and sedation induced by the α2-AR agonist medetomidine in dogs.{60727} It also prevents hypoalgesia induced by the non-steroidal anti-inflammatory drug (NSAID) ketoprofen in sheep.{60728} Atipamezole (0.3 mg/kg) enhances contralateral circling behavior induced by apomorphine or L-DOPA (Item No. 13248) and prolongs the duration of action of L-DOPA in a rat model of Parkinson’s disease.{25704} Formulations containing atipamezole have been used to reverse the sedative and analgesic effects of dexmedetomidine or medetomidine in dogs. Atipamezole is an imidazole that potently antagonizes the α2-adrenoceptor (Ki = 1.6 nM).{25705,25706} It shows selectivity over the α1-adrenoceptor (Ki = 13,300 nM) and is a poor antagonist at a wide variety of other receptors and channels.{25706} Through its effects at the α2-adrenoceptor, atipamezole reverses the sedative and analgesic effects of α2-adrenoceptor agonists, alters cognitive functions and sexual behavior, and has neuroprotective effects.{25706} It may also potentiate the effects of dopaminergic drugs used in Parkinson’s disease.{25706,25704}

Size	5 mg
Shipping	dry ice
CAS Number	104075-48-1
Molecular Formula	C₁₄H₁₆N₂ • HCl
SMILES	CCC1(C2=CN=CN2)CC3=CC=CC=C3C1.Cl
Molecular Weight	248,8
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.29
UNSPSC code	12352100

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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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