5-HYDROXY TRYPTAMINE, [³H]-

5-Hydroxytryptamine (5-HT, serotonin) is a neurotransmitter in the central nervous system (CNS). 5-HT binds 5-HT serotonin receptors to regulate smooth muscle in the cardiovascular system and the GI tract and enhances platelet aggregation. These receptors are part of a group of serotonin G-protein coupled receptors (GPCRs) found in the central and peripheral nervous systems. 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, PerkinElmer has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET1167:

1. Derek N. Middlemiss, John R. Fozard, 8-Hydroxy-2-(di-n-propylamino)-tetralin discriminates between subtypes of the 5-HT1 recognition site, In European Journal of Pharmacology, Volume 90, Issue 1, 1983, Pages 151-153.
2. Derek N. Middlemiss, Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol, In European Journal of Pharmacology, Volume 101, Issues 3–4, 1984, Pages 289-293.
3. Piñeyro Graciela, Castanon, Nathalie, Hen, René, Blier, Pierre, Regulation of [3H]5-HT release in raphe, frontal cortex and hippocampus of 5-HT1B knock-out mice, NeuroReport, Volume 7, Issue 1, 1995, Pages 353-359.