Atipamezole (hydrochloride)

Atipamezole is an antagonist of alpha2A-adrenergic receptors (alpha2A-ARs, Ki = 1.86 nM). It is selective for alpha2A-ARs over alpha2B- and alpha1-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 alpha2-AR agonist medetomidine in dogs. It also prevents hypoalgesia induced by the non-steroidal anti-inflammatory drug (NSAID) ketoprofen in sheep. Atipamezole (0.3 mg/kg) enhances contralateral circling behavior induced by apomorphine or L-DOPA (Cay-13248) and prolongs the duration of action of L-DOPA in a rat model of Parkinson's disease. 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 alpha2-adrenoceptor (Ki = 1.6 nM). It shows selectivity over the alpha1-adrenoceptor (Ki = 13,300 nM) and is a poor antagonist at a wide variety of other receptors and channels. Through its effects at the alpha2-adrenoceptor, atipamezole reverses the sedative and analgesic effects of alpha2-adrenoceptor agonists, alters cognitive functions and sexual behavior, and has neuroprotective effects. It may also potentiate the effects of dopaminergic drugs used in Parkinson's disease.Formal Name: 5-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole, monohydrochloride. CAS Number: 104075-48-1. Molecular Formula: C14H16N2 . HCl. Formula Weight: 248.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 10 mg/ml. lambdamax: 213 nm. SMILES: CCC1(C2=CN=CN2)CC3=CC=CC=C3C1.Cl. InChi Code: InChI=1S/C14H16N2.ClH/c1-2-14(13-9-15-10-16-13)7-11-5-3-4-6-12(11)8-14,/h3-6,9-10H,2,7-8H2,1H3,(H,15,16),1H. InChi Key: PCCVCJAQMHDWJY-UHFFFAOYSA-N.