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Data

Product overview

  • Name
    ZM 241385
  • Short description
    Potent, selective A2A receptor antagonist
  • Biological description

    ZM 241385 is a potent, selective adenosine A2A receptor inverse agonist (Ki values are <1, 50, 255 nM and >10 µM at A2A, A2B, A1 and A3 receptors respectively).


    The crystal structure of the human A2A receptor was determined in complex with ZM 241385.

    Activation of the A2A receptor enhances the release of glutamate, dopamine and acetylcholine and also inhibits GABA release.

    The A2AR has been shown to interact with various receptors including the mGlu5, D2R, A1R and CB1 receptors.

    A2A receptor activation modulates synaptic plasticity and neuronal excitability.


    ZM 241385 is active in vivo.

  • Alternative names
    ZM241385
  • Biological action
    Antagonist
  • Purity
    >99%
  • Citations

Properties

  • Chemical name
    4-(2-[7-Amino-2-(2-furyl)[1,2,4]tri azolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol
  • Molecular Weight
    337.34
  • Chemical structure
    ZM 241385 [139180-30-6]
  • Molecular Formula
    C16H15N7O2
  • CAS Number
    139180-30-6
  • PubChem identifier
    176407
  • SMILES
    C1=COC(=C1)C2=NN3C(=NC(=NC3=N2)NCCC4=CC=C(C=C4)O)N
  • Source
    Synthetic
  • InChi
    InChI=1S/C16H15N7O2/c17-14-20-15(18-8-7-10-3-5-11(24)6-4-10)21-16-19-13(22-23(14)16)12-2-1-9-25-12/h1-6,9,24H,7-8H2,(H3,17,18,19,20,21,22)
  • InChiKey
    PWTBZOIUWZOPFT-UHFFFAOYSA-N
  • MDL number
    MFCD00908394
  • Appearance
    White solid

Storing and Using Your Product

  • Storage instructions
    Room temperature
  • Solubility overview
    Soluble in DMSO (100 mM) and in ethanol (5 mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for ZM 241385

  • The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist.

    Jaakola et al (2008) Science 322 (5905) : 1211-7
    PubMedID: 18832607
  • Adenosine A(2A) receptors in psychopharmacology: modulators of behavior, mood and cognition.

    Shen and Chen (2009) Curr Neuropharmacol. 7(3) : 195-206
    PubMedID: 20190961
  • In vivo characterisation of ZM 241385, a selective adenosine A2A receptor antagonist.

    Keddie et al (1996) Eur J Pharmacol 301(1-3) : 107-13
    PubMedID: 8773453
  • The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosine receptor antagonist.

    Poucher et al (1995) Br J Pharmacol 115(6) : 1096-102
    PubMedID: 582508
  • Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.

    Ongini et al (1999) Naunyn Schmiedebergs Arch Pharmacol. 359(1) : 7-10
    PubMedID: 9933143
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