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ST1936

CAS No. : 1210-81-7

MCE 站：ST1936

产品活性：ST1936是一种选择性的纳摩尔亲和力的 5-HT₆ 受体激动剂，对人 5-HT₆、5-HT₇ 和 5-HT_2B 受体的 K_i 值分别为 13 nM，168 nM 和 245 nM。ST1936 对人和大鼠的 α2 肾上腺素受体也显示出中等亲和力 (K_i 为 300 nM)。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor  |  Adrenergic Receptor

In Vitro: ST1936 appears to be relatively selective for 5-HT₆ receptors, although it has shown affinity also for 5-HT_2B, 5-HT_1A, 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 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 reduces the frequency of spontaneous excitatory postsynaptic currents, with an IC₅₀ of 1.3 μM.

In Vivo: ST1936 (5, 10, 20 mg/kg; i.p.) 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.) 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.

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