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Atipamezole CAS: 104054-27-5

Category: Inhibitors
Product Name: Atipamezole
Cat No: I000237
CAS No: 104054-27-5
Molecular Formula: C14H16N2
Molecular Weight: 212.29
Solubility: DMSO: ≥30 mg/mL
Target: alpha2-adrenoceptor
CAS 104054-27-5,Atipamezole
  • Description

Atipamezole(MPV1248) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor. 

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]. 

  • References

[1]. Jager LP, et al. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6. 

[2]. Biegon A, et al. Quantitative in vitro and ex vivo autoradiography of the alpha 2-adrenoceptor antagonist [3H]atipamezole. Eur J Pharmacol. 1992 Nov 24;224(1):27-38. 

[3]. Virtanen R, et al. Highly selective and specific antagonism of central and peripheral alpha 2-adrenoceptors by atipamezole. Arch Int Pharmacodyn Ther. 1989 Jan-Feb;297:190-204.

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