Product Name | Atipamezole,MPV-1248,MPV1248,MPV 1248 |
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Product Description | Atipamezole(MPV1248) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor. IC50 value: Target: alpha2-adrenoceptor antagonist in vitro: The alpha2-adrenoceptor antagonist atipamezole was a potent inhibitor of aldosterone release (range 10-1000 nM) [1]. In receptor binding studies [( 3H]-clonidine and [3H]-prazosin displacement) an alpha 2/alpha 1 selectivity ratio of 8526 was obtained for atipamezole, while idazoxan and yohimbine showed ratios of 27 and 40, respectively. Atipamezole had also about a 100 times higher affinity on alpha 2-adrenoceptors than the reference compounds [3]. in vivo: In vivo studies of [3H]atipamezole demonstrated good penetration into the brain (0.3-1.8% injected dose/g at 5 min, depending upon brain region). In addition, [3H]atipamezole displayed rapid in vivo clearance of nonspecific binding such that at 1 h following an i.v. injection of the drug (100 microCi/animal, rat tail vein administration) the pattern of radioactivity in the brain correlated very well with the receptor distribution as seen by in vitro autoradiography [2]. In mice, medetomidine-induced sedation was effectively antagonized by atipamezole [3]. |
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Price | $450/50mg |
Specification | Numerous |
Product Review | 0 |
Vendor Information | MedChemExpress LLC http://www.medchemexpress.com 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Middlesex County New Jersey 08852 United States Phone: 609-228-6898 Fax: 609-228-5909 E-Mail: sales@medchemexpress.com |