FLA-797
FLA-797 is a brain-penetrant dopamine D2 receptor blocker and very low affinity for dopamine D1 receptors. FLA-797 selectively binds to and blocks postsynaptic dopamine D2 receptors. FLA-797 induces catalepsy in male rats. FLA-797 blocks dopamine agonist-induced hypothermia in male rats. FLA-797 contributes marginally to the dopamine D2 receptor-blocking activity of Remoxipride (HY-101313) in male rats. FLA-797 does not mimic the atypical antipsychotic profile of Remoxipride. FLA-797 can be used for research on mental disorders.
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- CAS No.: 84226-14-2
- Formule: C15H21BrN2O3
- Masse moléculaire:357.24
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
D2 Receptor |
D1 Receptor |
In Vitro
FLA-797 (60 min) shows high, selective affinity for dopamine D2 receptors (Ki = 0.49 nM) over D1 receptors in rat striatal homogenates[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
FLA-797 (0.02-20 μmol/kg; i.p.; single dose 60 minutes prior to Apomorphine (HY-12723)) potently blocks Apomorphine-induced hyperactivity (ED50 = 0.06 μmol/kg i.p.) and stereotypies in rats, demonstrating ~15-20-fold greater effectiveness than Remoxipride at blocking hyperactivity[2].
FLA-797 (0.01-1 μmol/kg; i.p.; single dose 30 minutes prior to apomorphine) blocks Apomorphine-induced hypothermia in rats with an ED50 of 0.3 μmol/kg i.p., showing ~3-fold greater effectiveness than Remoxipride[2].
FLA-797 (0.04-0.5 μmol/kg; i.p., s.c.; single dose 60 minutes prior to testing) potently blocks d-amphetamine-induced locomotion in rats, with an ED50 of 0.5 μmol/kg i.p. and 0.04 μmol/kg s.c., showing ~6-fold and ~25-fold greater effectiveness than Remoxipride via the respective routes[2].
FLA-797 (0.63-20 μmol/kg; i.p., s.c., i.v.; single dose) potently induces catalepsy in rats, with ED50 values ranging from <0.3 μmol/kg s.c. (grid test) to 3.1 μmol/kg i.p. (grid test), and is 40 to at least 200 times more effective than Remoxipride depending on administration route[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with Apomorphine 1 mg/kg s.c.)[2]
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Dosage: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;
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Administration:i.p.; single dose 60 minutes prior to apomorphine
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Result:Had an ED50 of 0.06 μmol/kg i.p.
for blocking Apomorphine-induced hyperactivity.
Had an ED50 of 0.32 μmol/kg i.p.
for blocking Apomorphine-induced oral stereotypies.
Was approximately 15-20 times more effective than Remoxipride at blocking hyperactivity, with a stereotypy/hyperactivity ratio of 5.3.
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Animal Model:Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with Apomorphine 1 mg/kg s.c.)[2]
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Dosage: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
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Administration:i.p.; single dose
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Result:Had an ED50 of 0.3 μmol/kg i.p.
for blocking Rpomorphine-induced hypothermia, making it approximately three times more effective than Remoxipride.
When administered 60 minutes prior to Apomorphine, its ED50 increased to ~1.7 μmol/kg i.p.
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Animal Model:Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with d-amphetamine 1.5 mg/kg i.p.)[2]
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Dosage:0.25 μmol/kg; 1 μmol/kg; 2.5 μmol/kg
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Administration:i.p.; single dose 60 minutes prior to testing
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Result:Had an ED50 of 0.5 μmol/kg
for blocking d-amphetamine-induced locomotion.
Was approximately six times more effective than Remoxipride via intraperitoneal administration.
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Animal Model:Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with d-amphetamine 1.5 mg/kg i.p.)[2]
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Dosage:0.01 μmol/kg; 0.05 μmol/kg; 0.1 μmol/kg; 0.25 μmol/kg; 1 μmol/kg
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Administration:s.c.; single dose 60 minutes prior to testing
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Result:Had an ED50 of 0.04 μmol/kg
for blocking d-amphetamine-induced locomotion.
Was approximately 25 times more effective via subcutaneous administration.
Completely suppressed d-amphetamine-induced motor activity at a dose of 0.25 μmol/kg s.c.
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Animal Model:Sprague-Dawley (male, 55-75 days old, 260-350 g)[2]
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Dosage:0.63 kg/μmol; 1.25 kg/μmol; 2.5 kg/μmol; 5 kg/μmol; 10 kg/μmol; 20 μmol/kg
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Administration:i.p.; single dose; s.c.; single dose; i.v.; single dose
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Result:Had ED50 values for inducing bar test catalepsy of 0.9 μmol/kg i.p., 0.5 μmol/kg s.c., and 0.6 μmol/kg i.v.
Had ED50 values for inducing vertical grid test catalepsy of 3.1 μmol/kg i.p., <0.3 μmol/kg s.c., and 0.4 μmol/kg i.v.
Was 40 to at least 200 times more effective than Remoxipride at inducing catalepsy depending on administration route, with a stereoselective effect (the (+)-isomer failed to induce catalepsy at 20 μmol/kg i.p.).
Produced immediate catalepsy lasting the full 240-minute observation period at a 20 μmol/kg i.p.
or 2.5 μmol/kg i.v.
dose.
Chemical Information
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CAS No. 84226-14-2
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Masse moléculaire 357.24
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Formule C15H21BrN2O3
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SMILES
CCN(CCC1)[C@@H]1CNC(C2=C(C=CC(Br)=C2O)OC)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Nilsson LB, et al. Optimization of a peak compression system for a remoxipride metabolite (FLA797) and its application to bioanalysis. J Chromatogr. 1992;591(1-2):207-217. [Content Brief]
[2]. Ogren SO, et al. Effects of remoxipride's metabolites on dopamine D2 receptors and receptor functions in the rat. Pharmacol Toxicol. 1993;73(6):325-334. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FLA-797 Related Classifications
HY-182381 Related Classifications
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Keywords
- FLA-797
- 84226-14-2
- FLA797
- FLA 797
- Dopamine Receptor
- postsynaptic dopamine D2 receptors
- dopamine D1 receptors
- blood-brain barrier
- dopamine D2 receptor
- rat striatal homogenates
- d-amphetamine-induced locomotion
- plasma
- apomorphine-induced hyperactivity
- male rats
- apomorphine-induced hypothermia
- Inhibitor
- inhibitor
- inhibit