Dexmedetomidine
The Chinese name is dexmedetomidine
dexmedetomidine
More English nicknames
Dexmedetomidine biological activity
Description Dexmedetomidine (+) -medetomidine is a potent, selective, and orally active alpha2 adrenergic receptor agonist with a Ki of 1.08 nM. Dexmedetomidine is 1620 times more selective to α1-adrenergic receptors. Dexmedetomidine has antianxiety, sedative and moderate analgesic effects [1][2][3].
Related category
Signal path > > G protein coupled receptor /G protein > > Adrenergic receptors
Research Field > > neuropathy
target
Alpha2-adrenergic receptor:1.08 nM (Ki)
In vitro studies, by substitution [3H] clonidine [1], metomidine was more selective to α2 adrenergic receptor (Ki=1.08 nM) than α1 adrenergic receptor (Ki=1750 nM) in the rat meninges. Metomidine (0.1-100nm) inhibited the tic response of the vas deferens in mice stimulated by the field, and pD2 was 9.0[1].
In vivo study of metomidine (10-100μg/kg; Intravenous injection at 5-minute intervals) produced dose-dependent pupil dilation in pentobarbital anesthetized rats [1]. Animal model: Female Sprague-Dawley rats (270-350 g) [1] Dose: 1,5,10,50,100 mg/kg intravenous infusion every 5 min Result: Pupil dilation of 2.5 mm (about half of the maximum effect) at a cumulative dose of 4μg/kg.
Reference literature
[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; 9 (1-2) : 150-14.
[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 to 40.
Physical and chemical properties of dexmedetomidine
Density 1.053g/cm3
The boiling point is 381.9ºC at 760mmHg
Melting point 146-149°C
Molecular formula C13H16N2
Molecular weight 200.28000
Flash point 191.3ºC
Accurate mass 200.13100
PSA 28.68000
LogP 3.17830
Vapor pressure 1.08E-05mmHg at 25°C
Refractive index 1.569
Dexmedetomidine Safety information
Customs Code: 2933290090
China
