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BRL 54443

CAS No. : 57477-39-1

MCE 站：BRL 54443

产品活性：BRL 54443 是 5-HT_1E/1F 受体激动剂，K_i 分别为 1.1 nM 和 0.7 nM，比对其它 5-HT 和多巴胺受体的抑制性高 30 倍以上。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Despite its low affinity for other receptors [5-HT_1A (63 nM), 5-HT_1B (126 nM), 5-HT_1D (63 nM), 5-HT_2A (1259 nM), 5-HT_2B (100 nM), 5-HT_2C (316 nM), 5-HT₆ (>10,000 nM), 5-HT₇ (>10,000 nM), D₂ (501 nM), D₃ (631 nM), and α_1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT_1F receptors.
In DG membranes, BRL54443 selectively stimulates 5-HT_1E receptors and potently inhibits forskolin-dependent cAMP production (IC₅₀=14 nM). BRL 54443 also induces contraction (-log EC₅₀=6.52).

In Vivo: Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats.

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