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Muscimol, 3-Hydroxy-5-Aminomethylisoxazole, [Methylene-3H(N)]-, 250µCi (9.25MBq)

3H Muscimol radioligand. Muscimol acts as a potent selective agonist at GABAA receptors. It also acts as a partial agonist at GABAA-rho receptors.

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NET574250UC
250 µCi
1752.00 USD
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NET574001MC
1 mCi
4383.00 USD
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Detail Information

Muscimol function as a potent selective agonist at GABAAreceptors. It binds to the same site on these receptors as GABA itself. Muscimol has minimal affinity for GABA uptake sites making it more attractive for receptor studies than GABA itself. It also acts as a partial agonist at GABAA-rho receptor. Muscimol is classified as an isoxazole; it displays sedatives-hypnotic, depressant and dissociative psychoactivity. When administered, it affects neuronal activity in multiple regions of the brain including the cerebral cortex, hippocampus and cerebellum.

We offer both agonist and antagonist radioligands for autoradiographic visualization or performing saturation and competition assays to determine receptor expression levels (Bmax), dissociation constants (Kd), association and dissociation rates (kon and koff), and inhibitor constants (Ki) for a variety of receptors. We develop our radioligands to the highest specific activity possible and provide high purity resulting in low non-specific binding products. Each of our ultra-pure radioligands is fully characterized for pharmacological action and validated in receptor binding assays.

Radiolabeled ligands remain the most sensitive method for probing receptor binding biology; yielding unprecedented sensitivity gives results that technicians and scientists can trust. For over 50 years, PerkinElmer has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET574:

  1. M. Rey, A.S. Veleiro, A.A. Ghini, M.S. Kruse, G. Burton, H. Coirini. Effect of synthetic steroids on GABAA receptor binding in rat brain. Neuroscience. April 2015. Volume 290, pages 138-146.
  2. Mariana Rey, Maria Sol Kruse, Lautaro D. Alvarex, Alberto A. Ghini, Adriana S. Veleiro, Gerardo Burton, Hector Coirini. Neuroprotective action of synthetic steroids with oxygen bridge. Activity on GABAA receptor. Experimental Biology. November 2013. Volume 249, pages 49-58.
  3. Mammele Stefana, Frauenknecht Katrina, Sevimli Sevgi, Diederich Kai, Bauer Henrike, Grimm Christina, Minnerup Jens, Schäbitz Wolf-Rüdiger, Sommer Clemens J. Restorative Neurology and Neuroscience. 2106. Volume 34, no. 4, pages 665-675

Specifications

Detection Method Radiometric
Label Position Nominally Labeled
Molecular Weight 114.1
Product Brand Name NEN Radiochemicals
Radioisotope H-3
Radionuclide 3H
Receptor Type Benzodiazepine, GABAA
Shipping Condition Dry Ice
Special Ordering Information This is a radioactive product - shipping address must have a license to receive radioactive materials.
Therapeutic Area CNS & Neurologic
Unit Size 250 µCi