Mesulergine, [N-methyl-³H]-

Mesulergine acts as an antagonist at serotonin 5-HT_2A and 5-HT_2C receptors, and as a partial agonist at dopamine receptors.

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 NET1148:

1. Dhwanil A. Dalwadi, Seongcheol Kim, Shahnawaz M. Amdani, Zhenglan Chen, Ren-Qi Huang, John A. Schetz, Molecular mechanisms of serotonergic action of the HIV-1 antiretroviral efavirenz, In Pharmacological Research, Volume 110, 2016, Pages 10-24.
2. Daniel Hoyer, Günter Engel, Hans O. Kalkman, Molecular pharmacology of 5-HT1 and 5-HT2 recognition sites in rat and pig brain membranes: Radioligand binding studies with [3H]5-HT, [3H]8-OH-DPAT, (−)[125I]iodocyanopindolol, [3H]mesulergine and [3H]Ketanserin, In European Journal of Pharmacology, Volume 118, Issues 1–2, 1985, Pages 13-23.