FLA-797 (60 min) showed high selective affinity for dopamine D2 receptors in rat striatal homogenate (Ki = 0.49 nM), but no affinity for D1 receptors [2].

Twenty minutes after intraperitoneal injection of 40 μmol/kg ramoxipride in rats, the plasma concentration of FLA-797 reached 0.6 nM[1]. FLA-797 (0.02-20 μmol/kg; intraperitoneal injection; single administration, 60 minutes before apomorphine administration) effectively blocked apomorphine-induced hyperactivity (ED50 = 0.06 μmol/kg, intraperitoneal injection) and stereotyped behaviors in rats, and its efficacy in blocking hyperactivity was about 15-20 times higher than that of ramoxipride[2]. FLA-797 (0.01-1 μmol/kg; intraperitoneal injection; single administration, 30 minutes before apomorphine administration) blocked apomorphine-induced hypothermia in rats, and its ED50 was 0.3 μmol/kg, which was about 3 times higher than that of ramoxipride[2]. FLA-797 (0.04-0.5 μmol/kg; intraperitoneal injection, subcutaneous injection; single administration, administered 60 minutes before the test) effectively blocked d-amphetamine-induced movement in rats, with ED50 values of 0.5 μmol/kg (intraperitoneal injection) and 0.04 μmol/kg (subcutaneous injection), respectively, which were about 6 times and 25 times more potent than ramoxipride, respectively [2]. FLA-797 (0.63-20 μmol/kg; intraperitoneal injection, subcutaneous injection, intravenous injection; single administration) effectively induced rigidity in rats, with ED50 values ranging from <0.3 μmol/kg (subcutaneous injection, grid test) to 3.1 μmol/kg (intraperitoneal injection, grid test), which were 40 times to at least 200 times more potent than ramoxipride, depending on the route of administration [2].

Animal/Disease Models:Sprague-Dawley mice (male, 55-75 days old, 260-350 g, subcutaneously injected with apomorphine 1 mg/kg) [2]
Doses: 0.02 μmol/kg; 0.05 μmol/kg; 0.1 μmol/kg; 0.2 μmol/kg; 0.5 μmol/kg; 1 μmol/kg; 2 μmol/kg; 5 μmol/kg; 10 μmol/kg; 20 μmol/kg;
Route of Administration: Intraperitoneal injection; a single dose 60 minutes before apomorphine injection.
Experimental Results: The ED50 for blocking apomorphine-induced ADHD by intraperitoneal injection was 0.06 μmol/kg. The ED50 for blocking apomorphine-induced oral stereotyped behaviors by intraperitoneal injection was 0.32 μmol/kg. Its effectiveness in blocking ADHD is about 15-20 times that of ramoxipride, and the stereotyped behavior/ADHD ratio is 5.3.

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Animal/Disease Models:Sprague-Dawley mice (male, 55-75 days old, 260-350 g, subcutaneously injected with apomorphine 1 mg/kg) [2]
Doses: 0.025 μmol/kg; 0.05 μmol/kg; 0.1 μmol/kg; 0.25 μmol/kg; 0.5 μmol/kg; 1 μmol/kg; 2.5 μmol/kg; 5 μmol/kg; 10 μmol/kg
Route of Administration: Intraperitoneal injection; single dose
Experimental Results: Intraperitoneal injection blocked the ED50 of ripomorphine-induced hypothermia at 0.3 μmol/kg, making it about 3 times more effective than rimoxipril. Administering the drug 60 minutes before intraperitoneal injection increased the ED50 to about 1.7 μmol/kg.

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Animal/Disease Models:Sprague-Dawley mice (male, 55-75 days old, 260-350 g, intraperitoneally injected with 1.5 mg/kg dextromethorphan) [2]
Doses: 0.25 μmol/kg; 1 μmol/kg; 2.5 μmol/kg
Route of Administration: Intraperitoneal injection; single dose, administered 60 minutes before the test
Experimental Results: The ED50 for blocking dextromethorphan-induced kinetic activity was 0.5 μmol/kg. This effect was approximately six times that of intraperitoneal ramoxipride.

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Animal/Disease Models:Sprague-Dawley mice (male, 55-75 days old, 260-350 g, intraperitoneally injected with 1.5 mg/kg dextromethorphan) [2]
Doses: 0.01 μmol/kg; 0.05 μmol/kg; 0.1 μmol/kg; 0.25 μmol/kg; 1 μmol/kg
Route of Administration: Subcutaneous injection; single dose administered 60 minutes before the test
Experimental Results: The ED50 for blocking dextromethorphan-induced kinesiology was 0.04 μmol/kg. The effect of subcutaneous administration was approximately 25 times that of intravenous administration. A subcutaneous dose of 0.25 μmol/kg completely inhibited dextromethorphan-induced kinesiology.

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Animal/Disease Models:Sprague-Dawley mice (male, 55-75 days old, 260-350 g) [2]
Doses: 0.63 kg/μmol; 1.25 kg/μmol; 2.5 kg/μmol; 5 kg/μmol; 10 kg/μmol; 20 μmol/kg
Route of Administration: Intraperitoneal injection; single dose; subcutaneous injection; single dose; intravenous injection; single dose
Experimental Results: The ED50 values for inducing rigidity in the rod test were: 0.9 μmol/kg for intraperitoneal injection, 0.5 μmol/kg for subcutaneous injection, and 0.6 μmol/kg for intravenous injection. The ED50 values for inducing rigidity in the vertical grid test were: 3.1 μmol/kg for intraperitoneal injection, <0.3 μmol/kg for subcutaneous injection, and 0.4 μmol/kg for intravenous injection. Depending on the route of administration, its potency in inducing rigidity is 40 to at least 200 times that of ramusxipride, and it exhibits stereoselectivity (the (+)- isomer failed to induce rigidity at an intraperitoneal dose of 20 μmol/kg). Rigidity is induced immediately at an intraperitoneal dose of 20 μmol/kg or an intravenous dose of 2.5 μmol/kg and persists throughout the 240-minute observation period.

[1]. Optimization of a peak compression system for a remoxipride metabolite (FLA797) and its application to bioanalysis. J Chromatogr. 1992;591(1-2):207-217.

[2]. Effects of remoxipride's metabolites on dopamine D2 receptors and receptor functions in the rat. Pharmacol Toxicol. 1993;73(6):325-334.

84226-14-2

Typically exists as solids at room temperature

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)