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

Muscimol function as a potent selective agonist at GABA_Areceptors. 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 GABA_A-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 (B_max), dissociation constants (K_d), association and dissociation rates (k_on and k_off), and inhibitor constants (K_i) 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, Revvity has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET574:

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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 GABA_A 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