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ZM241385

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Chemical Structure| 139180-30-6 同义名 : -
CAS号 : 139180-30-6
货号 : A132647
分子式 : C16H15N7O2
纯度 : 99%+
分子量 : 337.336
MDL号 : MFCD00908394
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Adenosine Receptor
描述 Adenosine modulates a variety of physiological functions acting via specific cell surface receptors which are divided into at least four subtypes: A1, A2a, A2b and A3. The A2a receptor subtype which is coupled to stimulation of adenylyl cyclase, is a high affinity receptor found in large amounts in the brain striatum. In the periphery, the A2a receptor is localized in different organs and tissues, including platelets, neutrophils and vascular smooth muscle cells [6]. ZM 241385 is a novel non-xanthine adenosine receptor antagonist with selectivity for the A2a receptor subtype [7]. In rat phaeochromocytoma cell membranes, ZM 241385 displaced binding of tritiated 5'-N-ethylcarboxamidoadenosine (NECA) with a pIC50 of 9.52. In guinea-pig isolated Langendorff hearts, ZM 241385 antagonized vasodilatation of the coronary bed produced by 2-chloroadenosine (2-CADO) and 2-[p-(2-carboxyethyl) phenethylamino]-5'-N-ethylcarboxamidoadenosine (CGS21680) with pA2 values of 8.57 and 9.02 respectively. It also antagonized the bradycardic action of 2-CADO in guinea-pig atria with a pA2 of 5.95 [7]. In the CA1 area of the rat hippocampus, which is the most sensitive region to ischemia, ZM241385, delay the appearance of anoxic depolarization (AD), protect from the synaptic activity depression brought about by a severe (7 min) OGD period, and protect CA1 neuron and astrocyte from injury [8].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.64mL

5.93mL

2.96mL
参考文献

[1]Wang Z, Che PL, Du J, Ha B, Yarema KJ. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385. PLoS One. 2010 Nov 8;5(11):e13883.

[2]Lasley RD, Kristo G, Keith BJ, Mentzer RM Jr. The A2a/A2b receptor antagonist ZM-241385 blocks the cardioprotective effect of adenosine agonist pretreatment in in vivo rat myocardium. Am J Physiol Heart Circ Physiol. 2007 Jan;292(1):H426-31.

[3]Keddie JR, Poucher SM, et al. In vivo characterisation of ZM 241385, a selective adenosine A2A receptor antagonist. Eur J Pharmacol. 1996 Apr 22;301(1-3):107-13.

[4]Fernández P, Trzaska S, et al. Pharmacological blockade of A2A receptors prevents dermal fibrosis in a model of elevated tissue adenosine. Am J Pathol. 2008 Jun;172(6):1675-82.

[5]Byeon JJ, Park MH, et al. In Vitro, In Silico, and In Vivo Assessments of Pharmacokinetic Properties of ZM241385. Molecules. 2020 Mar 2;25(5). pii: E1106.

[6]Varani K. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol. 1996 Apr;117(8):1693-701. doi: 10.1111/j.1476-5381.1996.tb15341.x.

[7] Poucher SM. The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosine receptor antagonist. Br J Pharmacol. 1995 Jul;115(6):1096-102.

[8]Pedata F. Adenosine A2A receptors modulate acute injury and neuroinflammation in brain ischemia. Mediators Inflamm. 2014;2014:805198. doi: 10.1155/2014/805198.