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Chemical Structure| 139180-30-6 Chemical Structure| 139180-30-6

Structure of ZM241385
CAS No.: 139180-30-6

Chemical Structure| 139180-30-6

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ZM241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.

Synonyms: ZM241385

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Product Details of ZM241385

CAS No. :139180-30-6
Formula : C16H15N7O2
M.W : 337.34
SMILES Code : OC1=CC=C(CCNC2=NC3=NC(C4=CC=CO4)=NN3C(N)=N2)C=C1
Synonyms :
ZM241385
MDL No. :MFCD00908394
InChI Key :PWTBZOIUWZOPFT-UHFFFAOYSA-N
Pubchem ID :176407

Safety of ZM241385

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Related Pathways of ZM241385

GPCR

Isoform Comparison

Biological Activity

Target
  • Adenosine Receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
CD3+CD4+ T lymphocytes 10 µM 24 hours ZM241385 blocked the inhibitory effect of zeatin riboside on proinflaμMatory cytokine production by CD3+CD4+ T lymphocytes. PMC4654369
CD3+CD8+ T lymphocytes 10 µM 24 hours ZM241385 blocked the inhibitory effect of zeatin riboside on proinflaμMatory cytokine production by CD3+CD8+ T lymphocytes. PMC4654369
CA3 pyramidal cells 50 nM 10 minutes ZM241385 rescued long-term potentiation (LTP) of A/C synapses in APP/PS1 mice PMC4915032
mouse neutrophils 30 and 300 µmol/l 6 hours To investigate the effect of ZM241385 on the interaction between A2AR and mGluR5, results showed that at glutamate concentrations of 30 and 300 µmol/l, ZM241385 inhibited the interaction between A2AR and mGluR5 and reduced the expression of inflaμMatory cytokines. PMC10725968
human neutrophils 300 µmol/l 6 hours To investigate the effect of ZM241385 on the interaction between A2AR and mGluR5, results showed that at a glutamate concentration of 300 µmol/l, ZM241385 inhibited the interaction between A2AR and mGluR5 and reduced the expression of inflaμMatory cytokines. PMC6603980
murine osteoblast precursors 1μM 24 hours To study the effect of ZM241385 on CGS21680-induced RANKL expression, results showed that ZM241385 reversed the inhibitory effect of CGS21680 on RANKL expression. PMC4476949
human mesenchymal stem cells 1μM 24 hours To study the effect of ZM241385 on CGS21680-induced OPG expression, results showed that ZM241385 reversed the enhancing effect of CGS21680 on OPG expression. PMC4476949

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice severe TBI-induced ALI model 50 mg/kg 5 days per week for 2 weeks To investigate the effect of ZM241385 on severe TBI-induced ALI, results showed that ZM241385 attenuated lung injury and neutrophil infiltration. PMC3620361
Mice Cd73-deficient mice Intraperitoneal and subcutaneous injection 1 mg/kg single dose, administered at 3 h after TBI To study the effect of ZM241385 on hypoxia-induced vascular leakage, results showed that ZM241385 significantly increased pulmonary vascular leakage and pulmonary edema. PMC1237012
C57BL/6 mice wear particle-induced osteolysis model local injection 60 mg/kg Single dose, 2 hours duration To study the effect of ZM241385 on MTX-induced inhibition of osteolysis, results showed that ZM241385 reversed the inhibitory effect of MTX on osteolysis. PMC4476949

Protocol

Bio Calculators
Preparing Stock Solutions 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

References

[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.

 

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