BRL 44408 (maleate)

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BRL 44408 (maleate)

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Cat No: 29454

Biochemicals - Receptor Pharmacology

BRL 44408 is an antagonist of α2A-adrenergic receptors (α2A-ARs; Ki = 8.56 nM for the recombinant human receptors).{45714} It is greater than 50-fold selective for α2A-ARs over α1-, α2B-, α2C-, β1-, and β2-ARs, as well as 19 other neurotransmitter rec...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole, 2Z-butenedioate

Correlated keywords:

118343-19-4 BRL44408 ?-2A ?2AAR 1 2B 2C ?-1 2 ?2AR anti-depressant paraphenylquinone

Product Overview:
BRL 44408 is an antagonist of α2A-adrenergic receptors (α2A-ARs; Ki = 8.56 nM for the recombinant human receptors).{45714} It is greater than 50-fold selective for α2A-ARs over α1-, α2B-, α2C-, β1-, and β2-ARs, as well as 19 other neurotransmitter receptors, transporters, and enzymes in a panel at 1 µM. BRL 44408 inhibits forskolin-stimulated cAMP accumulation with an IC50 value of 92.3 nM in CHO cells expressing the recombinant human α2A-AR. It increases norepinephrine and dopamine levels by 200 and 100%, respectively, in rat medial prefrontal cortex when administered at a dose of 10 mg/kg. BRL 44408 (10 and 30 mg/kg) decreases the time rats spend immobile in the forced swim test, indicating antidepressant-like activity, and reduces para-phenylquinone-induced abdominal stretching, indicating analgesic activity, in rats.

Size	5 mg
Shipping	dry ice
CAS Number	681806-46-2
Molecular Formula	C₁₃H₁₇N₃ • C₄H₄O₄
SMILES	CC1N(CC2=NCCN2)CC3=CC=CC=C31.OC(/C=C\C(O)=O)=O
Molecular Weight	331,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.29
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.

Accreditations
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.