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ST1936 oxalate

CAS No. : 1782228-83-4

MCE 站：ST1936 oxalate

产品活性：ST1936 oxalate 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 oxalate 对人 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

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.

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 ?g/kg for the SNc; 50–400 ?g/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.

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