A positive allosteric modulator of the GABAA receptor
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Tracazolate

Item No. 45457

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(butylamino)-1-ethyl-6-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ethyl ester
CAS Number
41094-88-6
Synonyms
  • ICI 136753
Molecular Formula
C16H24N4O2
Formula Weight
304.4
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=C(C1=C(C)N=C2C(C=NN2CC)=C1NCCCC)OCC
InChi Code
InChI=1S/C16H24N4O2/c1-5-8-9-17-14-12-10-18-20(6-2)15(12)19-11(4)13(14)16(21)22-7-3/h10H,5-9H2,1-4H3,(H,17,19)
InChi Key
PCTRYMLLRKWXGF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $99

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    5 mg

    $396

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    10 mg

    $594

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    25 mg

    $990

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    Product Description

    Tracazolate is a positive allosteric modulator of the GABAA receptor (GABAAR).1 It potentiates GABA-stimulated currents in X. laevis oocytes expressing α1β3γ2s and α1β1δ subunit-containing GABAARs (EC50s = 1.5 and 16.7 µM, respectively) and increases the maximal response to GABA in X. laevis oocytes expressing α1β1δ subunit-containing GABAARs, but reduces the maximal response to GABA in X. laevis oocytes expressing α1β3γ2s subunit-containing GABAARs. Tracazolate selectively potentiates GABA-induced currents in X. laevis oocytes expressing β3 over β1 subunit-containing GABAARs (EC50s = 1.5 and 13.2 µM for α1β3γ2s and α1β1γ2s subunit-containing GABAARs, respectively). Tracazolate (5 mg/kg) increases time spent in social interactions but does not reduce locomotor activity, indicating anxiolytic but not sedating activity, in rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Thompson, S.-A., Wingrove, P.B., Connelly, L., et al. Tracazolate reveals a novel type of allosteric interaction with recombinant γ-aminobutyric acidA receptors. Mol. Pharmacol. 61(4), 861-869 (2002).

    2. File, S.E., and Pellow, S. The anxiolytic but not the sedative properties of tracazolate are reversed by the benzodiazepine receptor antagonist, Ro 15-1788. Neuropsychobiology 14(4), 193-197 (1985).