GR 65630, [N-Methyl-³H]-, 25µCi (925kBq)

GR 65630 acts as an antagonist at the 5-HT₃ receptor. This receptor belongs to a family of ligand-gated ion channels and has effects on nausea on vomiting in the central nervous system, and emesis in the peripheral nervous system.

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, PerkinElmer has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET1011:

1. Wong, E. H. F., Bonhaus, D. W., Wu, I., Stefanich, E. and Eglen, R. M. (1993), Labelling of 5-Hydroxytryptamine3 Receptors with a Novel 5-HT3 Receptor Ligand, [3H]RS-42358–197. Journal of Neurochemistry, Volume 60, 1993, Pages 921–930.
2. I. Van Wijngaarden, M.Th.M. Tulp, W. Soudijn, The concept of selectivity in 5-HT receptor research, In European Journal of Pharmacology: Molecular Pharmacology, Volume 188, Issue 6, 1990, Pages 301-312.