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Dexmedetomidine

右旋美托咪啶

Mechanism of action:

Dexmedetomidine 是一種選擇性 α₂-腎上腺素受體促效劑(selective α₂-adrenergic receptor agonist),屬於咪唑(imidazole)衍生物,是美托咪啶(medetomidine)的 (S)-對映異構體,具右旋光性。Dexmedetomidine 能在腦幹藍斑核(locus coeruleus)活化 α₂A 受體,抑制正腎上腺素(norepinephrine)的釋放,降低交感神經活性,可引發鎮靜、鎮痛與抗焦慮相關作用。Dexmedetomidine 也會活化脊髓背角(dorsal horn)的 α₂ 受體,抑制神經傳遞物質(如 substance P)的釋放,減少疼痛訊號傳導,產生鎮痛相關作用。

​Reference(s):

1. Fairbanks CA et al. (2002). alpha(2C)-Adrenergic receptors mediate spinal analgesia and adrenergic-opioid synergy. J Pharmacol Exp Ther. 


2. Scheibner J et al. (2002). Alpha 2-adrenoceptors in the enteric nervous system: a study in alpha 2A-adrenoceptor-deficient mice. Br J Pharmacol.

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