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NLX-204

CAS No. : 2170405-10-2

MCE 站：NLX-204

产品活性：NLX-204 是一种具有口服活性、有效、高亲和力和选择性的 5-HT_1A 受体偏向激动剂 (pK_i=10.19)。NLX-204 对 α₁ 和 D₂ 受体的亲和力高于对其他脱靶受体的亲和力。NLX-204 可用于抗抑郁的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: NLX-204 (10 μM) shows substantial binding inhibition (higher than 50%) for adrenergic α_1A ａnd α_2A ａnd dopaminergic D_2S receptors. NLX-204 (1 μM) exhibits much lower binding inhibition at D₂ ａnd α_2A receptors but maintains a relatively high value for the α_1Areceptor. NLX-204 (0.1~10 μM) has a low propensity for hERG channel blockade ａnd suggests that the investigated series has a low risk with respect to hERG-related cardiac safety. NLX-204 also exhibits high microsomal stability. NLX-204 displays no P-gp inhibition (6.5% of inhibition at 10 μM) as well as negligible inhibition of CYP3A4 ａnd CYP2D6 (23.2 ａnd 15.9% at 10 μM, respectively). NLX-204 does not elicit flat body posture (FBP), a common side effect of the 5-HT_1A receptor stimulation, suggesting that its preference for activation of 5-HT_1A receptor-mediated ERK1/2 phosphorylation in vitro translates to preferential antidepressant effects rather than induction of ＇＇behavioral syndrome＇＇.

In Vivo: NLX-204 (2.5 mg/kg; p.o.) is rapidly absorbed from the gastrointestinal tract (Tmax = 15 min), reaches relatively high serum concentrations ａnd shows higher concentration than those in serum for all doses.
NLX-204 (0.04~2.5 mg/kg; p.o.) shows that statistically significant elevation of pERK1/2 is observed at the two highest doses (2.5 ａnd 0.63 mg/kg), but a tendency to increase pERK1/2 levels is also seen at lower doses.
NLX-204 robustly ａnd significantly increases rat PFC ERK1/2 phosphorylation in a time dependent manner.

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