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Etbicyphat

TMPP, Trimethylopropane phosphate, Ethyl bicyclic phosphate

An Antagonist of GABA(A) Receptors

Cat #: E-175
Alternative Name TMPP, Trimethylopropane phosphate, Ethyl bicyclic phosphate
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 178.12
    Purity: >98%
    Effective concentration 0.5-50 µM.
    Structure
    Chemical name 4-Ethyl-2,6,7-trioxa-1-phosphabicyclo[2.2.2]octane 1-oxide.
    Molecular formula C6H11O4P.
    CAS No.: 1005-93-2
    PubChem CID 13869
    Activity Etbicyphat, an ethyl bicyclophosphate organophosphorous compound, is a GABA receptor antagonist (KB = 3.98 µM for GABA(A) receptors),1 a blocker of neuronal voltage and GABA dependent Cl- currents, and a potent convulsant (≥0.4 mg/kg IP in rats) 2,3.
    References-Activity
    1. Higgins, G.M. and Gardier, R.W. (1990) Toxicol. Appl. Pharmacol. 105, 103.
    2. Rossi, J. et al. (2001) Prog. Neuropsychopharmacol. Biol. Psychiatry 25, 1323.
    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 Soluble in water. Centrifuge before use (10000 x g, 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs Etbicyphat inhibits GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs Etbicyphat inhibits GABA(A) receptors expressed in Xenopus oocytes.
      Representative time course of GABA(A) α1/β2 current, activated by a continuous application (top dotted line) of 0.1 µM γ-aminobutyric acid (#G-110), and inhibited by 2 µM and 10 µM Etbicyphat (#E-175), as indicated (bar), at a holding potential of -60 mV.
    References - Scientific background
    1. Rijal, S.O. and Gross, G.W. (2008) J. Neurosci. Methods 173, 183.
    2. Rossi, J. et al. (2001) Prog. Neuropsychopharmacol. Biol. Psychiatry 25, 1323.
    3. Rossi, J. et al. (1998) Drug Metab Dispos. 26,1058.
    4. Lindsey, J.W. et al. (1998) Neurotoxicology 19, 215.
    5. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol Biol. Psychiatry 56, 35.
    Scientific background

    Etbicyphat, also called trimethylopropane phosphate, is a synthetic convulsing compound that acts as a potent antagonist of GABA(A) receptors. TMPP acts through binding to the picrotoxinin and benzodiazepine receptor sites of the GABA(A) ionophore complex. TMPP is eliminated through the urine with no evidence of phase I or phase II metabolism and shows rapid clearance from the blood system1,2.

    Several studies showed that infusion of TMPP into the nucleus accumbens of adult rats induces subclinical seizures and hyperlocomotor activity3.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter, through the central nervous system and play an important role in inhibiting cell excitation in the central nervous system. The GABA(A) receptor is a major target of antiseizure drugs4.

    Target GABA(A) receptors
    Lyophilized Powder
    Last update: 25/07/2021

    Etbicyphat (#E-175) is a highly pure, synthetic, and biologically active compound.

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

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