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PU02

PU 02

A Negative Allosteric Modulator of 5-HT3

Cat #: P-165
Alternative Name PU 02
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 292.4
    Purity: >98%
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name 6-(naphthalen-1-ylmethylsulfanyl)-7H-purine.
    Molecular formula C16H12N4S.
    CAS No.: 313984-77-9
    PubChem CID 720937
    Activity PU02 is a negative allosteric modulator of 5-HT31.
    References-Activity
    1. Trattnig, S.M. et. al. (2012) J. Biol. Chem. 287, 25241.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 200 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs PU02 blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs PU02 blocks 5-HT3A receptors expressed in HEK 293T cells. 
      5-HT3A receptor currents were elicited by 10 µM 5-HT, delivered every 3 minutes. PU02 (#P-165) was applied 30 seconds before stimulation at 0.1, 1 and 10 µM as indicated and inhibited the 5-HT induced current in a dose dependent and reversible manner.
    References - Scientific background
    1. Hannon, J. et al. (2008) Behav. Brain Res. 195, 198.
    2. Trattnig, S.M. et al. (2012) J. Biol. Chem. 287, 25241.
    Scientific background

    Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid Tryptophan by the enzyme tryptophan-decarboxylase. The 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.

    PU02 is a synthetic, potent and selective negative allosteric modulator of the 5-HT3 receptor. PU02 has an effective concentration of 0.1-10 μM and an IC50 of approximately 1μM. PU02 acts through a transmembrane site situated between two subunits. The Ser248, Leu288, Ile290, Thr294, and Gly306 residues are identified as important molecular determinants of PU02 activity. It is suggested that the naphthalene group of PU02 docks into the hydrophobic cavity formed by these molecular determinants. Specific mutations of Ser248, Thr294, and Gly306 convert PU02 into a complex modulator, promoting and inhibiting 5-HT-evoked signaling through these mutated sites at low and high concentrations, respectively. The PU02 binding site in the 5-HT3 receptor corresponds to allosteric sites in other anionic Cys-loop receptors. The dramatic changes in the functional properties of PU02 induced by subtle changes in its binding site exhibit that delicate structural can alternate between allosteric inhibition and potentiation of 5-HT and other Cys-loop receptors2.

    Target 5-HT3 receptors
    Last update: 12/08/2021

    PU02 (#P-165) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information