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NLX-101 (F-15599)

Cat. No. M10608
NLX-101 (F-15599) Structure
Synonym:

NLX101

Size Price Availability
2mg USD 240  USD240 4-7 Days
10mg USD 630  USD630 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

NLX-101 (F-15599) is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM. NLX-101 (F-15599) mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors. NLX-101 (F-15599) has over 1000-fold higher affinity for this target over other receptors. 

F15599 (0.06 or 0.12 mg/kg) significantly reduces l-DOPA-induced dyskinesia (LID). F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, i,p,) results in a significant and dose-dependent (MED = 0.125 mg/kg) delay in the latency to attack, and a potent reduction (ID50 = 0.095 mg/kg) in the amount of aggressive behaviour directed towards the intruder rat. Starting from the 0.25 mg/kg dose, F15599 induces clear signs of the so-called serotonin syndrome characterized by flat body posture, head-waving, lower lip retraction and hindlimb abduction, leading to increased behavioural inactivity scores and social disengagement. F15599 increases dopamine output in mPFC (an effect dependent on the activation of postsynaptic 5-HT1A receptors) with an ED50 of 30 µg/kg i.p., whereas it reduces hippocampal 5-HT release (an effect dependent exclusively on 5-HT1A autoreceptor activation) with an ED50 of 240 µg/kg i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 394.85
Formula C19H21ClF2N4O
CAS Number 635323-95-4
Purity >99%
Solubility DMSO ≥ 90 mg/mL
Storage 2-8°C, protect from light, sealed
References

[1] R Depoortere, et al. Behav Brain Res. NLX-101, a highly selective 5-HT 1A receptor biased agonist, mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors

[2] Samantha M Meadows, et al. Exp Neurol. Characterizing the differential roles of striatal 5-HT 1A auto- and hetero-receptors in the reduction of l-DOPA-induced dyskinesia

[3] Sietse F de Boer, et al. Psychopharmacology (Berl). Anti-aggressive effects of the selective high-efficacy 'biased' 5-HT₁A receptor agonists F15599 and F13714 in male WTG rats

[4] Philippe Huot, et al. Neuropharmacology. The highly-selective 5-HT(1A) agonist F15599 reduces L-DOPA-induced dyskinesia without compromising anti-parkinsonian benefits in the MPTP-lesioned macaque

[5] L Llado-Pelfort, et al. Br J Pharmacol. Preferential in vivo action of F15599, a novel 5-HT(1A) receptor agonist, at postsynaptic 5-HT(1A) receptors

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Keywords: NLX-101 (F-15599), NLX101 supplier, 5-HT Receptor, inhibitors

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