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