2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. 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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FLA-797

FLA-797 Chemical Structure

CAS No. : 84226-14-2

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FLA-797 Related Antibodies

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Description

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[1][2].

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.

FLA-797 Related Antibodies
In Vivo

FLA-797 reaches a plasma concentration of 0.6 nM at 20 minutes post-dose following intraperitoneal administration of 40 μmol/kg Remoxipride to rats[1].
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.

Animal Model: Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with Apomorphine 1 mg/kg s.c.)[2]
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;
Administration: i.p.; single dose 60 minutes prior to apomorphine
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.
Animal Model: Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with Apomorphine 1 mg/kg s.c.)[2]
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
Administration: i.p.; single dose
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.
Animal Model: Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with d-amphetamine 1.5 mg/kg i.p.)[2]
Dosage: 0.25 μmol/kg; 1 μmol/kg; 2.5 μmol/kg
Administration: i.p.; single dose 60 minutes prior to testing
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.
Animal Model: Sprague-Dawley (male, 55-75 days old, 260-350 g, challenged with d-amphetamine 1.5 mg/kg i.p.)[2]
Dosage: 0.01 μmol/kg; 0.05 μmol/kg; 0.1 μmol/kg; 0.25 μmol/kg; 1 μmol/kg
Administration: s.c.; single dose 60 minutes prior to testing
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.
Animal Model: Sprague-Dawley (male, 55-75 days old, 260-350 g)[2]
Dosage: 0.63 kg/μmol; 1.25 kg/μmol; 2.5 kg/μmol; 5 kg/μmol; 10 kg/μmol; 20 μmol/kg
Administration: i.p.; single dose; s.c.; single dose; i.v.; single dose
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.
Molecular Weight

357.24

Formula

C15H21BrN2O3
CAS No.
SMILES

CCN(CCC1)[C@@H]1CNC(C2=C(C=CC(Br)=C2O)OC)=O
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Storage

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Purity & Documentation
References
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FLA-797 Related Classifications

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Keywords:

FLA-79784226-14-2FLA797FLA 797Dopamine Receptorpostsynaptic dopamine D2 receptorsdopamine D1 receptorsblood-brain barrierdopamine D2 receptorrat striatal homogenatesd-amphetamine-induced locomotionplasmaapomorphine-induced hyperactivitymale ratsapomorphine-induced hypothermiaInhibitorinhibitorinhibit

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