2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Adrafinil

Adrafinil (CRL 40028) is an orally active vigilance promoting agent. Adrafinil enhances central noradrenergic transmission, improves spontaneous activity, exploratory behavior, discriminative learning ability and response motivation, but impairs visuospatial working memory. Adrafinil antagonizes Prazosin (HY-B0193)-induced hypoactivity and hypothermia, exerts anticonvulsant effects, and induces sustained enhancement of high-frequency electrocortical activity. Adrafinil can be used for research on decreased alertness and specific cognitive deficits.

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Adrafinil

Adrafinil Chemical Structure

CAS No. : 63547-13-7

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Description

Adrafinil (CRL 40028) is an orally active vigilance promoting agent. Adrafinil enhances central noradrenergic transmission, improves spontaneous activity, exploratory behavior, discriminative learning ability and response motivation, but impairs visuospatial working memory. Adrafinil antagonizes Prazosin (HY-B0193)-induced hypoactivity and hypothermia, exerts anticonvulsant effects, and induces sustained enhancement of high-frequency electrocortical activity. Adrafinil can be used for research on decreased alertness and specific cognitive deficits[1][2][3][4].

In Vivo

Adrafinil (20 mg/kg; p.o.; daily; 2 hours before testing) significantly improves discrimination learning in aged beagle dogs, as measured by reduced errors and trials to criterion, without a significant effect on overall response latency[1].
Adrafinil (10-20 mg/kg; p.o.; single daily dose; 8 consecutive days) at 20 mg/kg significantly impairs visuospatial working memory in aged beagle dogs as measured by increased errors on the DNMP task, while 10 mg/kg adrafinil does not produce a significant change in task performance[2].
Adrafinil (16 mg/kg; i.p.; single dose) significantly antagonizes prazosin-induced hypomotility in male NMRI mice[3].
Adrafinil (2-8 mg/kg; i.p.; single dose) produces a significant, dose-dependent antagonism of prazosin-induced hypothermia in male NMRI mice[3].
Adrafinil (128 mg/kg; i.p.; single dose) significantly reduces handling-induced convulsive seizures in C57BL/6J quaking mice, with mean post-treatment seizures decreasing to 2.2 ± 1.13 from a pre-treatment mean of 10.9 ± 0.72 (p < 0.001), and this protective effect is antagonized by prazosin co-administration[3].
Adrafinil (10-50 mg/kg; p.o.; single dose) produces a significant, dose- and time-dependent increase in open field locomotion in aged Beagle dogs, with no induction of stereotypical behavior[4].
Adrafinil (10-40 mg/kg; p.o.; daily; 14 consecutive days) produces a dose-dependent increase in locomotor activity in aged Beagle dogs with repeated daily administration for 14 days, and response variability correlates with differences in adrafinil metabolism[4].
Adrafinil (20 mg/kg; p.o.; single dose prior to testing) at 20 mg/kg significantly improves discrimination learning and performance motivation in aged Beagle dogs relative to placebo[4].

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

Animal Model: Beagle (5 females, 3 males, 7.5 to 10 years old)[1]
Dosage: 20 mg/kg
Administration: p.o.; single dose; 2 hours before each behavioral test session
Result: Reduced errors to criterion compared to placebo.
Reduced trials to criterion compared to placebo.
Reduced unresponsive trials from 19.2% to 4% in a subject with motivation deficits under placebo.
Did not produce a statistically significant overall effect on response latency.
Animal Model: Beagle (aged, 8 female, 10 male, 9-12 years old)[2]
Dosage: 10 mg/kg; 20 mg/kg
Administration: p.o.; single daily dose; 8 consecutive days
Result: Produced no significant change in error rate compared to placebo at 10 mg/kg.
Significantly impaired visuospatial working memory, with significantly more total errors over the 8-day test period compared to both 10 mg/kg adrafinil and placebo at 20 mg/kg.
Caused impaired performance in both poor and good baseline performer groups at 20 mg/kg, with poor performers exhibiting a significant difference in errors between 10 mg/kg and 20 mg/kg doses.
Did not alter response latency to task stimuli at either dose level.
Animal Model: NMRI (male, 21-23 g)[3]
Dosage: 16 mg/kg
Administration: i.p.; single dose
Result: Restored motor activity to levels significantly higher than prazosin-only treatment.
Animal Model: NMRI (male, 21-23 g)[3]
Dosage: 2 mg/kg; 4 mg/kg; 8 mg/kg
Administration: i.p.; single dose
Result: Restored rectal temperatures to levels significantly higher than prazosin-only treatment.
Produced a significant, dose-dependent antagonism of prazosin-induced hypothermia, with the magnitude of recovery increasing with higher doses.
Animal Model: C57BL/6J quaking (male or female, 20-22 g, handling-induced convulsive seizures model)[3]
Dosage: 128 mg/kg (seizure reduction); 16 mg/kg, 32 mg/kg, 64 mg/kg (no effect)
Administration: i.p.; single dose
Result: Reduced mean seizure count from 10.9 before treatment to 2.2 after treatment.
Failed to produce a significant reduction in seizure counts at doses of 16, 32, and 64 mg/kg.
Had its protective effect against seizures clearly antagonized by co-administration of prazosin.
Animal Model: Beagle dogs (both sexes, 7 years of age or older)[4]
Dosage: 10 mg/kg; 30 mg/kg; 50 mg/kg
Administration: p.o.; single dose
Result: Produced a significant increase in locomotion relative to placebo, with effects that were dose-dependent and time-dependent.
Decreased urination frequency significantly only at the 50 mg/kg dose.
Induced no stereotypical behavior.
Animal Model: Beagle dogs (9 to 16 years of age)[4]
Dosage: 10 mg/kg; 20 mg/kg; 30 mg/kg; 40 mg/kg
Administration: p.o.; daily; 14 consecutive days
Result: Reliably increased locomotor activity at doses of 20, 30, and 40 mg/kg, with effects that were dose-dependent.
Generally induced no stereotypical behavior, though some individual dogs showed no response or decreased locomotion.
Decreased urination frequency only at the 40 mg/kg dose.
Caused a dose-dependent increase in serum levels at 2 hours post-dosing; at 10 hours, 40 mg/kg group levels were lower than the 10 mg/kg group (non-significant).
Dogs that showed increased activity had higher serum levels at 2 hours post-treatment and lower levels at 10 hours compared to non-responders.
Animal Model: Beagle dogs (7 to 10 years of age)[4]
Dosage: 20 mg/kg
Administration: p.o.; single dose prior to testing
Result: Significantly improved discrimination learning performance relative to placebo, with fewer errors and fewer trials to reach criterion.
Improved performance motivation and reduced day-to-day response variability in one dog with response failures under placebo.
Animal Model: Beagle dogs (over 10 years of age)[4]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: p.o.; daily; 3 consecutive days; 8 consecutive days
Result: Induced an arousal-type EEG state in all three dogs, characterized by increased alpha and beta activity and decreased delta and theta activity, with effects lasting for 4 hours post-administration.
Showed no differences in EEG effects between the 10, 20, and 40 mg/kg doses.
Caused a greater increase in alpha and beta activity in dogs with baseline EEG dominated by lower frequencies (delta, theta) than dogs with higher baseline alpha/beta activity.
Molecular Weight

289.35

Formula

C15H15NO3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NO)CS(C(C1=CC=CC=C1)C2=CC=CC=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (345.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4560 mL 17.2801 mL 34.5602 mL
5 mM 0.6912 mL 3.4560 mL 6.9120 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (17.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (17.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.85%

SDS (392 KB)

COA (250 KB) HNMR (155 KB) LCMS (103 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4560 mL 17.2801 mL 34.5602 mL 86.4006 mL
5 mM 0.6912 mL 3.4560 mL 6.9120 mL 17.2801 mL
10 mM 0.3456 mL 1.7280 mL 3.4560 mL 8.6401 mL
15 mM 0.2304 mL 1.1520 mL 2.3040 mL 5.7600 mL
20 mM 0.1728 mL 0.8640 mL 1.7280 mL 4.3200 mL
25 mM 0.1382 mL 0.6912 mL 1.3824 mL 3.4560 mL
30 mM 0.1152 mL 0.5760 mL 1.1520 mL 2.8800 mL
40 mM 0.0864 mL 0.4320 mL 0.8640 mL 2.1600 mL
50 mM 0.0691 mL 0.3456 mL 0.6912 mL 1.7280 mL
60 mM 0.0576 mL 0.2880 mL 0.5760 mL 1.4400 mL
80 mM 0.0432 mL 0.2160 mL 0.4320 mL 1.0800 mL
100 mM 0.0346 mL 0.1728 mL 0.3456 mL 0.8640 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Adrafinil63547-13-7CRL 40028CRL40028CRL-40028Adrenergic ReceptorBeta Receptoraged beagle dogsage-related cognitive declineα1 noradrenergic receptorC57BL/6J quaking micevisuospatial working memoryconvulsionsnoradrenergic transmissionage-associated cognitive impairmentdiscrimination learningmale NMRI miceInhibitorinhibitorinhibit

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