1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. NLX-204

NLX-204 

Cat. No.: HY-124631
Handling Instructions

NLX-204 is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 can be used for the research of antidepressant.

For research use only. We do not sell to patients.

NLX-204 Chemical Structure

NLX-204 Chemical Structure

CAS No. : 2170405-10-2

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Description

NLX-204 is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 can be used for the research of antidepressant[1].

IC50 & Target[1]

5-HT1A Receptor

10.19 (pKi)

In Vitro

NLX-204 (10 μM) shows substantial binding inhibition (higher than 50%) for adrenergic α1A and α2A and dopaminergic D2S receptors. NLX-204 (1 μM) exhibits much lower binding inhibition at D2 and α2A receptors but maintains a relatively high value for the α1Areceptor. 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-HT1A receptor stimulation, suggesting that its preference for activation of 5-HT1A receptor-mediated ERK1/2 phosphorylation in vitro translates to preferential antidepressant effects rather than induction of ''behavioral syndrome''[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
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[1].
NLX-204 robustly and significantly increases rat PFC ERK1/2 phosphorylation in a time dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (170~200 g)[1]
Dosage: 2.5 mg/kg
Administration: P.o.
Result: Rapidly absorbed from the gastrointestinal tract (Tmax = 15 min) and reached relatively high serum concentrations.
Animal Model: Male Wistar rats (170~200 g)[1]
Dosage: 2.5 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: The concentration of NLX-204 in brain tissue was higher than those in serum for all doses.
Animal Model: Male Wistar rats (170~200 g)[1]
Dosage: 0.04~2.5 mg/kg
Administration: P.o.
Result: Statistically significant elevation of pERK1/2 was observed at the two highest doses (2.5 and 0.63 mg/kg), but a tendency to increase pERK1/2 levels was also seen at lower doses.
Molecular Weight

409.86

Formula

C₂₀H₂₂ClF₂N₃O₂

CAS No.
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NLX-204
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HY-124631
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