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

FLA-797 是一种可穿透血脑屏障的多巴胺 D2 受体阻滞剂，对多巴胺 D1 受体的亲和力极低。FLA-797 可选择性结合并阻断突触后多巴胺 D2 受体。FLA-797 可诱导雄性大鼠出现僵住症。FLA-797 可阻断多巴胺激动剂诱导的雄性大鼠体温过低。FLA-797 对雄性大鼠中 Remoxipride (HY-101313) 的多巴胺 D2 受体阻断活性仅起到微弱作用。FLA-797 无法模拟 Remoxipride 的非典型抗精神病药特征。FLA-797 可用于精神障碍的研究。

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FLA-797

FLA-797 Chemical Structure

CAS No. : 84226-14-2

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FLA-797 相关抗体

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

FLA-797 (60 分钟) 在大鼠纹状体匀浆中对多巴胺 D2 受体表现出高选择性亲和力 (Ki = 0.49 nM)，其亲和力远高于对 D1 受体的亲和力[2]。

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

FLA-797 相关抗体:
体内研究
(In Vivo)

FLA-797 在给大鼠腹腔注射 40 μmol/kg remoxipride 后 20 分钟时，血浆浓度达 0.6 nM[1]。
FLA-797 (0.02-20 μmol/kg；腹腔注射；Apomorphine (HY-12723) 给药前 60 分钟单次给药) 可强效阻断大鼠中 Apomorphine 诱导的过度活动 (ED50 = 0.06 μmol/kg i.p.) 与刻板行为，其阻断过度活动的效力比 Remoxipride 高约 15-20 倍[2]。
FLA-797 (0.01-1 μmol/kg；腹腔注射；单剂量，于 Apomorphine 给药前 30 分钟给予) 可阻断大鼠由 Apomorphine 诱导的低体温，其腹腔注射 ED50 为 0.3 μmol/kg，效力比 Remoxipride 高约 3 倍[2]。
FLA-797 (0.04-0.5 μmol/kg；腹腔注射、皮下注射；测试前 60 分钟单次给药) 可强效阻断大鼠中 d-苯丙胺诱导的运动行为，其腹腔注射的 ED50 为 0.5 μmol/kg，皮下注射的 ED50 为 0.04 μmol/kg，经相应给药途径的效力分别比 Remoxipride 高约 6 倍和 25 倍[2]。
FLA-797 (0.63-20 μmol/kg；腹腔注射、皮下注射、静脉注射；单次给药) 可强效诱导大鼠出现僵住症，其 ED50 值范围为皮下注射<0.3 μmol/kg (网格试验) 至腹腔注射 3.1 μmol/kg (网格试验)，且根据给药途径的不同，其效力是 Remoxipride 的至少 40-200 倍[2]。

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.
分子量

357.24

Formula

C15H21BrN2O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

FLA-797 相关分类

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  • 稀释计算器

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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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产品名称：
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目录号：
HY-182381
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