The Sound of Evolution
Dexmedetomidine
Mechanism of action:
Dexmedetomidine is a selective α₂-adrenergic receptor agonist and an imidazole derivative. It is the (S)-enantiomer of medetomidine and is dextrorotatory. Dexmedetomidine activates α₂A receptors in the locus coeruleus of the brainstem, suppressing norepinephrine release and reducing sympathetic nervous system activity, which produces sedation, analgesia, and anxiolytic-related effects. It also activates α₂ receptors in the dorsal horn of the spinal cord, inhibiting the release of neurotransmitters such as substance P, thereby reducing pain signal transmission and producing analgesic-related effects.
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.