ST1936 oxalate

ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human α2 adrenergic receptor[1].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

5-HT6 Receptor:13 nM (Ki)

Human 5-HT7 Receptor:168 nM (Ki)

5-HT2B Receptor:245 nM (Ki)

ST1936 appears to be relatively selective for 5-HT6 receptors, although it has shown affinity also for 5-HT2B, 5-HT1A, 5-HT7 receptor and α-adrenergic receptors when tested in a broad crossreactivity panel that comprised G-protein-coupled receptors, ion channel binding sites, enzymes, and transporters[1].

In-vivo electrophysiological studies are performed to investigate the physiological role of 5-HT6 receptors in the control of the function of the substantia nigra pars compacta (SNc) and ventral tegmental area (VTA). Extracellular single-unit recordings are performed from putative dopamine-containing neurons in the SNc and VTA of anesthetised rats (Male Sprague-Dawley rats). In the SNc, acute systemic administration of ST1936 (Intravenous injection; 50–1600 µg/kg for the SNc; 50–400 µg/kg for the VTA) has no effects on basal firing activity of these dopamine neurons; however, in the VTA, ST1936 induces either dose-related increases (45% of cells) or decreases in basal activity of these dopaminergic neurons[1].

[1]. Borsini F, et al. Effects of ST1936, a selective serotonin-6 agonist, on electrical activity of putative mesencephalic dopaminergic neurons in the rat brain. J Psychopharmacol. 2015 Jul;29(7):802-11.