Ditolylguanidine acts as an agonist at sigma receptors (σ1 and σ2), and has neuroprotective and antidepressant effects.

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 NET986:

1. Dhwanil A. Dalwadi, Seongcheol Kim, John A. Schetz, Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia, In Neurochemistry International, Volume 105, 2017, Pages 21-31.
2. Diaz, J. L.; Christmann, U.; Fernandez, A.; Torrens, A.; Port, A.; Pascual, R.; Alvarez, I.; Burgueno, J.; Monroy, X.; Montero, A. Synthesis and Structure-Activity Relationship Study of a New Series of Selective σ1 Receptor Ligands for the Treatment of Pain: 4-Aminotriazoles J. Med. Chem. 2015, 58, Pages 2441– 2451.