Atipamezole (hydro<wbr>chloride)

Atipamezole (hydrochloride)

CAT N°: 9001181
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108.00 91.80

Atipamezole is an antagonist of ?2A-adrenergic receptors (?2A-ARs; Ki = 1.86 nM).{25705,25706} It is selective for ?2A-ARs over ?2B- and ?1-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 ?2-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 ?2-adrenoceptor (Ki = 1.6 nM).{25705,25706} It shows selectivity over the ?1-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 ?2-adrenoceptor, atipamezole reverses the sedative and analgesic effects of ?2-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}

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