Dexmedetomidine 是选择性、具有口服活性的 α2 肾上腺素能受体激动剂,Ki=1.08 nM。它对 α1 肾上腺素受体显示出 1620 倍的选择性。它具有抗焦虑活性,可用于研究促进睡眠和缓解疼痛。
产品描述
Dexmedetomidine is a Central alpha-2 Adrenergic Agonist. The mechanism of action of dexmedetomidine is as an Adrenergic alpha2-Agonist. The physiologic effect of dexmedetomidine is by means of General Anesthesia.
体外活性
Dexmedetomidine has a relatively high ratio of α2/α1-activity (1620:1 as compared with 220:1 for clonidine) and, therefore, is considered a full agonist of the α2 receptor. This may result in more potent effects of sedation without unwanted cardiovascular effects from α1 receptor activation. The 2-h half-life of dexmedetomidine is nearly 4-fold shorter than that of clonidine, which increases the likelihood that a continuous infusion of dexmedetomidine might be useful for sedation. Dexmedetomidine also has minimum alveolar anesthetic concentration (MAC)-sparing properties, but its use as an anesthetic adjuvant has been complicated by persistent hypotension that has mandated IV fluid administration and vasopressor administration. In addition, its use in large doses is complicated by hypertension from α2 receptor-mediated vascular constriction.
Cas No.
113775-47-6
分子式
C13H16N2
分子量
200.285
储存和溶解度
DMSO:40 mg/mL (199.72 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years