| 货号 | 16454-5mg |
| 描述 | Medetomidine is an imidazole derivative that acts as a selective agonist of α2-adrenoceptors (Ki = 1.08 nM vs. 1750 nM for α1-adrenoceptors).1,2 Medetomidine is a mixture of D and L isomers, with the D form, known as dexmedetomidine (Item No. 15581), described as the active form. Through its effect on α2-adrenoceptors, medetomidine has sedative, antinociceptive, analgesic, and hypothermic actions.3,4 Its effects on pain are additive or synergistic with fentanyl-type opioids.5,6 The effects of medetomidine are effectively countered by α2-adrenoceptor antagonists, like atipamezole.7 Selective α2-adrenoceptor agonists, including medetomidine, have anesthetic sparing properties, greatly reducing the dose of anesthetic required following premedication with the α2-adrenoceptor agonist.4 |
| 别名 | Domitor®;MPV 785; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Savola, J.M.,Ruskoaho, H.,Puurunen, J., et al. Evidence for medetomidine as a selective and potent agonist at α2-adrenoreceptors. J.Auton.Pharmacol. 6, 275-284 (1986). 2.Virtanen, R.,Savola, J.M.,Saano, V., et al. Characterization of the selectivity, specificity and potency of medetomidine as an α2-adrenoceptor agonist. Eur. J. Pharmacol. 150(1-2), 9-14 (1988). 3.Hunter, J.C.,Fontana, D.J.,Hedley, L.R., et al. Assessment of the role of α2-adrenoceptor subtypes in the antinociceptive, sedative and hypothermic action of dexmedetomidine in transgenic mice. British Journal of Pharmacology 122(7), 1339-1344 (1997). 4.Sinclair, M.D. A review of the physiological effects of α2-agonists related to the clinical use of medetomidine in small animal practice. Can.Vet.J. 44(11), 885-897 (2003). 5.Meert, T.F. and de Kock, M. Potentiation of the analgesic properties of fentanyl-like opioids with α2-adrenoceptor agonists in rats. Anesthesiology 81(3), 677-688 (1994). 6.Ossipov, M.H.,Harris, S.,Lloyd, P., et al. Antinociceptive interaction between opioids and medetomidine: Systemic additivity and spinal synergy. Anesthesiology 73(6), 1227-1235 (1990). 7.Scheinin, H.,Aantaa, R.,Anttila, M., et al. Reversal of the sedative and sympatholytic effects of dexmedetomidine with a specific α2-adrenoceptor antagonist atipamezole: A pharmacodynamic and kinetic study in healthy volunteers. Anesthesiology 89(3), 574-584 (1998). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 236.7 |
| CAS号 | 86347-15-1 |
| 稳定性 | ≥ 2 years |
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