Atipamezole hydrochloride


CAS No. : 104075-48-1

Atipamezole hydrochloride,104075-48-1
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000238
Synonyms:5-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole hydrochloride
Molecular Formula:C14H16N2 • HCl
Molecular Weight:248.8
Target:Adrenergic Receptor
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Appearance:Solid powder
Purity: > 98%


Cat No:I000238
Cas No:104075-48-1
Product-Name:Atipamezole hydrochloride
InChI: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
InChIKey:PCCVCJAQMHDWJY-UHFFFAOYSA-N
SMILES:CCC1(C2=CN=CN2)CC3=CC=CC=C3C1.Cl

Atipamezole hydrochloride(cas 104075-48-1) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.
IC50 value:

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].

1: Bush M, Raath JP, Phillips LG, Lance W. Immobilisation of impala (Aepyceros melampus) with a ketamine hydrochloride/medetomidine hydrochloride combination, and reversal with atipamezole hydrochloride. J S Afr Vet Assoc. 2004 Mar;75(1):14-8. PubMed PMID: 15214689.
2: Pettifer GR, Dyson DH, McDonell WN. An evaluation of the influence of medetomidine hydrochloride and atipamezole hydrochloride on the arrhythmogenic dose of epinephrine in dogs during halothane anesthesia. Can J Vet Res. 1996 Jan;60(1):1-6. PubMed PMID: 8825986; PubMed Central PMCID: PMC1263792.
3: Rioja E, Kerr CL, Enouri SS, McDonell WN. Sedative and cardiopulmonary effects of medetomidine hydrochloride and xylazine hydrochloride and their reversal with atipamezole hydrochloride in calves. Am J Vet Res. 2008 Mar;69(3):319-29. doi: 10.2460/ajvr.69.3.319. PubMed PMID: 18312129.
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