CRL-40,941 (Fladrafinil) , ≥98%

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Eugeroic related to Adrafinil. Weak Dopamine Reuptake Inhibitor (DRI). Psychotonic.

Chemical Name2-{[Bis(4-fluorophenyl)methyl]sulfinyl}-N-hydroxyacetamide
SynonymsFladrafinil, Fluorafinil, 2-(bis(4-fluorophenyl)methylsulfinyl)-N-hydroxyacetamide
CAS #90212-80-9
FormWhite to pale cream powder.
Molecular FormulaC15H13F2NO3S
Molecular Weight325.33 g/mol
Solubility Poorly soluble in water; Soluble to 5 mg / mL in ethanol; Soluble to 10 mg / mL in isopropanol.

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Precaution and Disclaimer:

This Material is Sold For Research Use Only. Terms of Sale Apply. Not for Human Consumption, nor Medical, Veterinary, or Household Uses.

Chemical Information:

CAS Number:90212-80-9
Purity:≥98%
Molecular Weight:325.33 g/mol
Melting Point:90-91°C
Molecular Formula:C15H13F2NO3S
Synonyms: 2-{[Bis(4-fluorophenyl)methyl]sulfinyl}-N-hydroxyacetamide, Fladrafinil, Fluorafinil, 2-(bis(4-fluorophenyl)methylsulfinyl)-N-hydroxyacetamide, 90212-80-9
PubChem CID:13316557
SMILES:C1=CC(=CC=C1C(C2=CC=C(C=C2)F)S(=O)CC(=O)NO)F

Technical Information:

Application:CRL-40,941 (Fladrafinil) is an eugeroic related to and of higher potency than adrafinil, with anticonflict properties.
Appearance:White to pale cream powder
Physical State:Solid
Solubility:Poorly soluble in water; Soluble to 5 mg / mL in ethanol; Soluble to 10 mg / mL in isopropanol
Storage:Store at room temperature or cooler, in a sealed airtight container, protected from heat, light and humidity.
Stability:Stable for at least two years when stored as above.

Background:

CRL-40,941 (Fladrafinil) is a psychotonic and eurgeroic (wakefulness-promoting substance) that is related to Adrafinil and CRL-40,940, with similar but more potent effects demonstrated in animal models.[1] Fladrafinil is the bis(p-fluoro) derivative of Adrafinil, and is, therefore, often referred to as “Fladrafinil”. Unfortunately, very little literature currently exists for this compound.

Unlike its parent compound, CRL-40, 941 also appears to demonstrate some interesting anti-aggressive (calming) properties in animal studies – according to the original 1983 patent filed by the Parisian Laboratoire L. Lafon.[1] In the late 1970s, this French laboratory was where compounds such as Modafinil, CRL-40-940, and CRL-40,941 were initially developed as a family of eugeroics, with research led by Dr. Michel Jouvet. 

The research team at Laboratoire Lafon observed that CRL-40,941 had similar psychotonic and eurgeroic properties as Adrafinil – albeit with improved bioavailability through oral administration. The unique characteristic of CRL-40,941 is its anti-aggressive properties in animal models, which sets it apart from both Modafinil and Adrafinil. 

An excerpt from the original CRL-40,941 patent states that:

CRL 40,941,as a psychotonic agent, is clearly more effective by the oral route, in the rat and in man, than [Adrafinil]. From the clinical point of view, CRL 40,941 acts at doses which are half those of [Adrafinil]. Excellent results were obtained in man when [CRL 40,941] was administered per os, at the rate of 2 to 3 capsules or tablets, (each containing 50mg of active ingredient) per day, particularly for 2 to 8 weeks in the treatment of hypersomnia and psychastenia.” [1]

In a recent (2017) study, researchers from Ireland studied the thermal degradation properties of several eugeroic agents including Modafinil, Adrafinil, CRL-40,940, and CRL-40,941. Their study produced interesting findings relating to the results of thermal degradation of Nootropics. They “identified a common GC injector port thermolysis product in the analysis of modafinil, adrafinil and modafinic acid” and proposed a mechanism for its formation. Furthermore, they found that CRL-40,940, CRL-40,941 and modafiendz produced the same degradant profile – which could lead to difficulties during forensic analysis.[2]

Modes of action:

The modes of action have not yet been fully determined for CRL-40,941.

Further Scientific research:

For more information, please consult the PubMed database.

Clinical Reviews:

As a result of the relative lack of research on this compound, there are no literature reviews or meta-analyses available at this time.

Human studies:

No human studies have been performed using this compound. 

Animal studies:

The results of a variety of animal studies on mice were included in the original CRL-40,941 patent. The research team at Laboratoire L. Lafon made several observations relating to the compound’s effects in mice:

  • The LD-0 (maximum non-lethal dose) of CRL-40,941 by the I.P. route in the male mouse is higher than 512 mg/kg.
  • One third of the mice receiving a very large dosage (1024 mg/kg I.P.) of CRL-40,941 presented abdominal cramps, depressed respiration, and sedation 45 minutes after administration, then died 24 hours after administration.
  • CRL 40,941 partially counteracted the hypothermia-inducing action of Oxotremorine.
  • Unlike other similar compounds, CRL-40,941 did not provoke any major motorial deficit, and did not increase the convulsant effects of electric shock.
  • Furthermore, it enabled a clear resumption of activity in the mouse habituated to its enclosure, improved motorial recovery in mice whose motility had been reduced by hypoxia, and counteracted sleep induced by barbital.
  • The compound appeared to potentiate the amphetaminic stereotypes after injection of 2 mg/kg amphetamine. [1]

 

Toxicity Cases:

No toxicity cases have been reported for this compound. 

Precaution and Disclaimer:
This Material is Sold For Research Use Only. Terms of Sale Apply.
Not for Human Consumption, nor Medical, Veterinary, or Household Uses.

References:

  • [1] Lafon, Louis (Paris, FR). (1983). Halogenobenzhydrylsulfinylacetohydroxamic acids - United States Patent 4489095. Available online from: http://www.freepatentsonline.com/4489095.html
  • [2] Dowling, G., Kavanagh, P. V., Talbot, B., O’Brien, J., Hessman, G., McLaughlin, G., … Brandt, S. D. (2016). Outsmarted by nootropics? An investigation into the thermal degradation of modafinil, modafinic acid, adrafinil, CRL-40,940 and CRL-40,941 in the GC injector: formation of 1,1,2,2-tetraphenylethane and its tetra fluoro analog. Drug Testing and Analysis, 9(3), 518–528.

Precaution and Disclaimer:

This Material is Sold For Research Use Only. Terms of Sale Apply. Not for Human Consumption, nor Medical, Veterinary, or Household Uses.