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1782228-83-4

1782228-83-4 structure
1782228-83-4 structure
  • Name: ST1936 oxalate
  • Chemical Name: ST1936 oxalate
  • CAS Number: 1782228-83-4
  • Molecular Formula: C15H19ClN2O4
  • Molecular Weight: 326.78
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2020-04-17 10:46:13
  • Modify Date: 2024-01-11 10:34:49
  • 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].

Name ST1936 oxalate
Description 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].
Related Catalog
Target

5-HT6 Receptor:13 nM (Ki)

Human 5-HT7 Receptor:168 nM (Ki)

5-HT2B Receptor:245 nM (Ki)

In Vitro 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 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].
References

[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.

Molecular Formula C15H19ClN2O4
Molecular Weight 326.78