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NLX-101, formerly known as F-15599, is a G-protein biased compound that activates serotonin 5-HT1A receptors with exceptional selectivity, having over 1000-fold higher affinity for this target over other receptors. Furthermore, NLX-101 functions as a "biased agonist" at 5-HT1A receptors, activating them preferentially in the parts of the brain that regulate mood and cognition.
| Targets |
5-HT1A Receptor ( Ki = 3.4 nM )
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|---|---|
| ln Vivo |
F15599 (0.06 or 0.12 mg/kg) dramatically lessens l-DOPA-induced dyskinesia (LID) in rats without impairing their ability to move. At a high dose of 30 μg/μL, rats treated with F15599 exhibit mild 5-HT syndrome and less LID[1]. F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, i,p) causes a strong reduction (ID50 = 0.095 mg/kg) in the amount of aggressive behavior aimed at the intruder rat, as well as a notable and dose-dependent delay (MED = 0.125 mg/kg) in the latency to attack. F15599 causes obvious symptoms of the so-called serotonin syndrome, which includes flat body posture, head waving, lower lip retraction, and hindlimb abduction, starting at a dose of 0.25 mg/kg. This results in higher behavioral inactivity scores and social disengagement[2]. F15599 decreases the discharge rate of dorsal raphe 5-hydroxytryptaminergic neurones at doses >10-fold higher (minimum effective dose 8.2 µg/kg i.v.) and increases the discharge rate of pyramidal neurones in the medial prefrontal cortex (mPFC) from 0.2 µg/kg i.v. F15599 has an ED50 of 30 µg/kg i.p. that increases dopamine output in mPFC, which is dependent on postsynaptic 5-HT1A receptor activation. On the other hand, it has an ED50 of 240 µg/kg i.p. that decreases hippocampal 5-HT release, which is solely dependent on 5-HT1A autoreceptor activation[3].
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| Animal Protocol |
In summary, this model involves housing male rats alone in sizable observation cages measuring 80 × 55 × 50 cm, along with an oviduct-ligated female, to prevent social isolation and promote sexual behavior, which in turn encourages territorial behavior. A baseline level of aggressive and offensive behavior is assessed after a week, three days in a row, during a maximum 10-minute confrontation with a male conspecific who is not known to the subject (WTG rats). About 60 minutes before the start of this social provocation test, the female partner of the experimental rat is taken out of the home observation cage. As conspecific intruder animals, naive male WTG rats (average weight 372 ± 9.5 g, 3.5–4 months old) are socially housed in groups of three in transparent Makrolon type IV cages. The intruder is eliminated during the first three tests as soon as the resident launches their first complete attack, and the attack latency time (ALT) is recorded. The fourth baseline test, which is conducted on day 4, records and analyzes the entire spectrum of behaviors. Based on the ALT and the degree of offensive behavior, the experimental groups are matched. The experimental groups contain only animals that have attacked (ALT <600 s). Eleven of the fourteen4 participants in the study are not attackers. The following day, day 5, the experimental vehicle (sterile Ultra Pure water, n = 19 and n = 20) or F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, IP, experiment 1, n = 45) or F13714 (0.003, 0.006, 0.012, 0.025, 0.062, 0.125, 0.250, IP, experiment 2, n = 50) are given 30 minutes prior to the 10-minute confrontation with a drug-free unfamiliar intruder conspecific, and their behavior is recorded once more. In addition, animals are tested in experiment 3 thirty minutes after treatment with vehicle/vehicle (UP), vehicle/F15599 (0.1 mg/kg) or F13714, or vehicle/WAY-100635 (0.3 mg/kg) or vehicle or WAY100635 (0.3 mg/kg)/F15599 (0.1 mg/kg) or F13714. There are 6–8 subjects in each treatment group, for a total of 41 creatures.
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| References |
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| Molecular Formula |
C19H21CLF2N4O
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|---|---|
| Molecular Weight |
394.85
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| Exact Mass |
394.137
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| Elemental Analysis |
C, 57.80; H, 5.36; Cl, 8.98; F, 9.62; N, 14.19; O, 4.05
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| CAS # |
635323-95-4
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| Related CAS # |
635323-95-4
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| PubChem CID |
11741361
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| Appearance |
White to off-white solid powder
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| LogP |
3.64
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
496
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C([H])=C([H])C(=C1[H])C(N1C([H])([H])C([H])([H])C(C([H])([H])N([H])C([H])([H])C2N=C([H])C(C([H])([H])[H])=C([H])N=2)(C([H])([H])C1([H])[H])F)=O)F
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| InChi Key |
WAAXKNFGOFTGLP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21ClF2N4O/c1-13-9-24-17(25-10-13)11-23-12-19(22)4-6-26(7-5-19)18(27)14-2-3-16(21)15(20)8-14/h2-3,8-10,23H,4-7,11-12H2,1H3
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| Chemical Name |
(3-chloro-4-fluorophenyl)-[4-fluoro-4-[[(5-methylpyrimidin-2-yl)methylamino]methyl]piperidin-1-yl]methanone
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| Synonyms |
NLX-101; NLX 101; NLX101; F-15,599; F 15,599; F15,599; F15599
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~250 mg/mL (~633.2 mM)
Ethanol: ~79 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5326 mL | 12.6630 mL | 25.3261 mL | |
| 5 mM | 0.5065 mL | 2.5326 mL | 5.0652 mL | |
| 10 mM | 0.2533 mL | 1.2663 mL | 2.5326 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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