PeptideDB

Dexmedetomidine

CAS: 113775-47-6 F: C13H16N2 W: 200.28

Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.
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Bioactivity Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
Invitro Medetomidine has high selectivity for α2 adrenoceptors (Ki=1.08 nM) over α1 adrenoceptors (Ki=1750 nM) in rat brain membranes as measured by the displacement of [3H]clonidine[1].Medetomidine (0.1-100 nM) inhibits the twitch response in field-stimulated mouse vas deferens, with a pD2 of 9.0[1].
In Vivo Medetomidine (10-100 μg/kg; i.v. at 5-min intervals) produces a dose-dependent pupillary dilatation in pentobarbitone-anaesthetized rats[1]. Animal Model:
Name Dexmedetomidine
CAS 113775-47-6
Formula C13H16N2
Molar Mass 200.28
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Reference [1]. Virtanen R, et, al. Characterization of the selectivity, specificity and potency of medetomidine as an alpha 2-adrenoceptor agonist. Eur J Pharmacol. 1988 May 20;150(1-2):9-14. [2]. Gertler R, et, al. Dexmedetomidine: a novel sedative-analgesic agent. Proc (Bayl Univ Med Cent). 2001 Jan;14(1):13-21. [3]. Sajid B, et, al. A comparison of oral dexmedetomidine and oral midazolam as premedicants in children. J Anaesthesiol Clin Pharmacol. Jan-Mar 2019;35(1):36-40.