同义名 :	-
	CAS号 :	59263-76-2
	货号 :	A302225
	分子式 :	C15H24ClNO
	纯度 :	99%+
	分子量 :	269.81
	MDL号 :	MFCD00941476
	存储条件：	Pure form Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Meptazinol Hydrochloride (Meptazinol) is a new opioid-type analgesic with mixed agonist/antagonist properties. It may be given orally, intravenously or intramuscularly[3]. Meptazinol is an agonist-antagonist opioid analgesic believed to be unique in its selectivity for mu1 (high affinity) receptors and its cholinergic activity[4]. Meptazinol inhibits a portion of 3H-labeled opiate and opioid peptide binding quite potently, with IC50 value under 1 nM[5]. Meptazinol and its isomers have anti-nociceptive and anti-hyperalgesic properties with the former more potent. The effects are mainly mediated by mu opioid receptors[6]. The intravenous administration, to anaesthetized rats, of meptazinol (1 and 2 mg kg-1), a partial agonist at opiate receptors, greatly reduced the incidence of ventricular extrasystoles that resulted from acute coronary artery occlusion. Moreover, pretreatment with meptazinol (1 and 2 mg kg-1) also reduced ventricular arrhythmias, including fibrillation, in conscious rats subjected to coronary artery occlusion[7].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.71mL 0.74mL 0.37mL	18.53mL 3.71mL 1.85mL	37.06mL 7.41mL 3.71mL

参考文献

[1]Shi Z, Zhang Q, et al. Pharmacokinetic behavior in plasma, cerebrospinal fluid and cerebral cortex after intranasal administration of hydrochloride meptazinol. Life Sci. 2005 Sep 30;77(20):2574-83. [2]Spiegel K, Pasternak GW. Meptazinol: a novel Mu-1 selective opioid analgesic. J Pharmacol Exp Ther. 1984 Feb;228(2):414-9. [3]Holmes B, Ward A. Meptazinol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy. Drugs. 1985 Oct;30(4):285-312 [4]Kaiko RF, Wallenstein SL, Rogers AG, Canel A, Jacobs B, Houde RW. Intramuscular meptazinol and morphine in postoperative pain. Clin Pharmacol Ther. 1985 May;37(5):589-96 [5]Spiegel K, Pasternak GW. Meptazinol: a novel Mu-1 selective opioid analgesic. J Pharmacol Exp Ther. 1984 Feb;228(2):414-9 [6]Wang PF, Zhang YQ, Qiu ZB, Zhao ZQ. Antinociceptive effects of meptazinol and its isomers on carrageenan-induced thermal hyperalgesia in rats. Sheng Li Xue Bao. 2004 Jun 25;56(3):295-300 [7]Fagbemi O, Kane KA, Leprán I, Parratt JR, Szekeres L. Antiarrhythmic actions of meptazinol, a partial agonist at opiate receptors, in acute myocardial ischaemia. Br J Pharmacol. 1983 Mar;78(3):455-60