GABAA and GABAC receptor agonist
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Analytical Standard(s)
38030Muscimol (CRM)
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Muscimol

Item No. 13667

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(aminomethyl)-3(2H)-isoxazolone
CAS Number
2763-96-4
Synonyms
  • Agarin
  • NSC 333569
  • Pantherine
Molecular Formula
C4H6N2O2
Formula Weight
114.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): 10 mg/mlWater: 50 mg/ml
SMILES
OC1=NOC(CN)=C1
InChi Code
InChI=1S/C4H6N2O2/c5-2-3-1-4(7)6-8-3/h1H,2,5H2,(H,6,7)
InChi Key
ZJQHPWUVQPJPQT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    10 mg

    $132

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    25 mg

    $310

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    Product Description

    Muscimol is a full GABAA agonist and partial GABAC agonist. It binds GABAA on both high- and low-affinity sites (Kd = 10 and 270 nM, respectively), stimulating chloride efflux with an EC50 value of 200 nM.1 Benzodiazepines enhance the effects of muscimol via GABAA without altering its binding.1,2 Muscimol activates GABAC receptors with an EC50 value of 1.3 μM.3 It also acts as an inhibitor of GABAA uptake and a substrate for the GABA-metabolizing enzyme GABA transaminase.4 Muscimol impairs memory formation and retrieval in mice and attenuates airway constriction in guinea pigs in vivo.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dunn, S.M., and Thuynsma, R.P. Reconstitution of purified GABAA receptors: Ligand binding and chloride transporting properties. Biochemistry 33(3), 755-763 (1994).

    2. Parramón, M., González, M.P., and Oset-Gasque, M.J. Pharmacological modulation of adrenal medullary GABAA receptor: Consistent with its subunit composition. Br. J. Pharmacol. 116, 1875-1881 (1995).

    3. Zhang, D., Pan, Z.H., Awobuluyi, M., et al. Structure and function of GABAc receptors: A comparison of native versus recombinant receptors. Trends Pharmacol. Sci. 22(3), 121-132 (2001).

    4. Krogsgaard-Larsen, P., Frolund, B., and Frydenvang, K. GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects. Curr. Pharm. Des. 6, 1193-1209 (2000).

    5. Jafari-Sabet, M., and Jannat-Dastjerdi, I. Muscimol state-dependent memory: Involvement of dorsal hippocampal μ-opioid receptors. Behav. Brain Res. 202, 5-10 (2009).

    6. Gleason, N.R., Gallos, G., Zhang, Y., et al. The GABAA agonist muscimol attenuates induced airway constriction in guinea pigs in vivo. J. Appl. Physiol. (1985) 106, 1257-1263 (2009).