5-CT, [³H]

5-CT is a tryptamine derivative closely related to serotonin. 5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. These receptors are part of a group of serotonin G-protein coupled receptors (GPCRs) found in the central and peripheral nervous systems, and modulate the release of neurotransmitters and hormones. 5-HT receptors are the pharmacological target of many antidepressants, antipsychotic, anti-migraine, and other pharmaceutical drugs.

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 NET1188:

1. G. Satała, B. Duszyńska, T. Lenda, G. Nowak, A. J. Bojarski. Allosteric Inhibition of Serotonin 5-HT7 Receptors by Zinc Ions, Molecular Neurobiology, 2017, pages 1-14.
2. K.W. Andressen, A. H. Ulsund, K. A. Krobert, M. J. Lohse, M. Bünemann, F. O. Levy, Related GPCRs couple differently to Gs: preassociation between G protein and 5-HT7 serotonin receptor reveals movement of Gαs upon receptor activation, FASEB, 2017.