Dexmedetomidine

113775-47-6

200.28

10 mM in DMSO

GPCR/G Protein; Neuronal Signaling

Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of alpha2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against alpha1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects.
In Vitro: Medetomidine has high selectivity for alpha2 adrenoceptors (Ki=1.08 nM) over alpha1 adrenoceptors (Ki=1750 nM) in rat brain membranes as measured by the displacement of [3H]clonidine.

Medetomidine (0.1-100 nM) inhibits the twitch response in field-stimulated mouse vas deferens, with a pD2 of 9.0.
In Vivo: Medetomidine (10-100 ug/kg; i.v. at 5-min intervals) produces a dose-dependent pupillary dilatation in pentobarbitone-anaesthetized rats.