Methylspiperone, [N-Methyl-³H]-, 250µCi (9.25MBq)

Methylspiperone functions as an antagonist for both the 5-HT_2A serotonin receptor and D_2/3 dopamine receptor. It shows low affinity for α₁-adrenergic receptors. Methylspiperone can be used as a PET tracer used to image D_2/3 and 5HT_2A receptor densities.

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 NET856:

1. Nathalie Schmieg, Cristina Rocchi, Stefania Romeo, Roberto Maggiom Mark J. Millan, Clotilde Mannoury la Cour. Dysbindin-1 modifies signaling and cellular localization of recombinant, human D_{3 and D2 receports. Journal of Neurochemistry, Volume 136, Issue 5, March 2016, pages 1037-1051.}
2. Dhwanil A. Dalwadi, Seongcheol Kim, Shahnawaz M. Amdani, Zhenglan Chen, Ren-Qi Huang, John A. Schetz. Molecular mechanisms of serotonergice action of the HIV-1 antiretrovial efavirenze. Pharmacological Research, volume 10, August 2016, pages 10-24
3. Sehyoun Yoon, Mi-Hyun Choi, Ja-Hyuan Baik. Wnt ligan binding to and regulation of dopamine D_{2 receptors. Dopamine Receptor Technologies. Neuromethods, vol 96,November 2014, pages 65-78}