Dexmedetomidine is a potent, selective, and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. It demonstrates 1620-fold selectivity against α1-adrenoceptor, exhibiting anxiolysis, sedation, and modest analgesia effects.
- Potent and selective α2-adrenoceptor agonist (Ki = 1.08 nM)
- Demonstrates 1620-fold selectivity against α1-adrenoceptor
- Exhibits anxiolysis, sedation, and modest analgesia effects
- EC50 of 1.5 nM for agonist activity at human recombinant alpha2A adrenergic receptor
- Inhibits twitch response in field-stimulated mouse vas deferens with pD2 of 9.0
- Produces dose-dependent pupillary dilatation in rats