ST1936 oxalate

SKU: orb1218621

Description

ST1936 oxalate is a selective, nanomolar affinity agonist of 5-HT6 receptor(Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively).

Key Properties

• CAS Number: 1782228-83-4
• MW: 326.78
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₉ClN₂O₄
• SMILES: CC1=C(C2=C(N1)C=CC(=C2)Cl)CCN(C)C.C(=O)(C(=O)O)O
• Target: 5-HT Receptor

Bioactivity

• In Vivo:
  ST1936 (5, 10, 20 mg/kg; i.p.) oxalate increases in a dose dependent manner extracellular dopamine (DA) and NA levels in the prefrontal cortex (PFCX). ST1936 (5, 10, 20 mg/kg; i.p.) oxalate increases extracellular DA and NA levels in the nucleus accumbens (NAc) core. Doses of 10 mg/kg increases dialysate DA (peak: 179%) while higher dose increases both DA and NA dialysates (201% and 231%, respectively). Doses of 5 mg/kg does not produce any effect.
• In Vitro:
  ST1936 oxalate 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. ST1936 oxalate behaves as a full 5-HT6 agonist on cloned cells and is able to increase Ca2+ concentration, phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 that is a downstream target of Fyn kinase. ST1936 oxalate reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC50 of 1.3 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor