2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GlyT
  4. Org 24461

Org 24461 是一种具有选择性且可穿透血脑屏障的 GlyT-1 抑制剂。Org 24461 可阻断甘氨酸的摄取、重摄取、反向转运、[3H]甘氨酸外流与释放。Org 24461 可增强 NMDA 受体功能，调节纹状体单胺/谷氨酸水平，并逆转 PCP 诱导的行为及脑电图异常。Org 24461 可用于视网膜缺氧/缺血及精神分裂症的相关研究。

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Org 24461

Org 24461 Chemical Structure

CAS No. : 372198-80-6

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Org 24461 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [3H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia[1][2][3][4][5].

IC50 & Target[1]

GLT1

 

体外研究
(In Vitro)

Org 24461 (40 min) 可强效抑制稳定表达 hGlyT-1b 的 CHO 细胞对甘氨酸的摄取，其 IC50 为 100 nM[1][2]。
Org 24461 (0.1-30 μM; 20 min) 可逆转 7-Chlorokynurenic acid (HY-100811) 诱导的离体鸡视网膜中 NMDA 介导的扩散性抑制潜伏期延长，其 IC50 为 0.36 μM；且在无 7-Chlorokynurenic acid 存在的情况下，10-30 μM 浓度可缩短 NMDA (HY-17551) 诱导的扩散性抑制潜伏期[1]。
Org 24461 (0.3 mM; 90 min) 可强效抑制氧糖剥夺诱导的离体鸡视网膜中 [3H]甘氨酸释放，但对常氧条件下的基础甘氨酸外流无影响[2]。
Org 24461 (预孵育 5 分钟；37°C 孵育 10 分钟) 可强效抑制大鼠大脑皮层突触体 (IC50 = 1.3 μM) 和大鼠纹状体突触体 (IC50 = 1.8 μM) 中高亲和力 [3H]甘氨酸的摄取[3]。
Org 24461 可抑制大鼠海马体 P2 突触体中 [3H]甘氨酸的摄取；在低 [3H]甘氨酸浓度下其 IC50 为 2.5 μM，在高 [3H]甘氨酸浓度下其 IC50 为 28 μM[4]。
Org 24461 不影响灌流大鼠海马脑片中的自发性 [3H]甘氨酸外流，但可抑制同一标本中甘氨酸刺激的 [3H]甘氨酸外流[4]。

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

Org 24461 相关抗体:
体内研究
(In Vivo)

Org 24461 (10 mg/kg；腹腔注射；单次给药) 可显著降低清醒大鼠纹状体细胞外多巴胺浓度，而对谷氨酸或丝氨酸水平无影响[3]。
Org 24461 (10 mg/kg；腹腔注射；单次给药；与 Risperidone (HY-11018) 1 mg/kg 腹腔注射联合给药) 可使清醒大鼠纹状体细胞外多巴胺浓度恢复正常，维持细胞外甘氨酸浓度处于升高状态，并显著提高细胞外谷氨酸浓度[3]。
Org 24461 (2-8 mg/kg；腹腔注射；单次给药) 可抑制 PCP 诱导的雄性 NMRI 小鼠高活动性，其腹腔注射 ID50 为 3.8 mg/kg[4]。
Org 24461 (3-30 mg/kg；腹腔注射；单次给药) 可抑制 D-苯丙胺诱导的雄性 NMRI 小鼠运动过度，其腹腔注射 ID50 为 13.5 mg/kg[4]。
Org 24461 (1-10 mg/kg；腹腔注射；单次给药) 可呈剂量依赖性逆转 PCP 诱导的清醒雄性 Wistar 大鼠脑电图功率谱变化[4]。
Org 24461 (10 mg/kg；静脉注射；单次给药) 可显著逆转 L-701324 (HY-18698) 诱导的大鼠中缝背核单个神经元放电频率降低[5]。

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

Animal Model: NMRI (male, 25-33 g, phencyclidine/PCP-induced hypermotility model)[4]
Dosage: 2 mg/kg; 4 mg/kg; 8 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently inhibited PCP-induced hypermotility, with an ID50 value of 3.8 mg/kg i.p.
Animal Model: NMRI (male, 25-33 g, D-amphetamine-induced hypermotility model)[4]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently inhibited D-amphetamine-induced hypermotility, with an ID50 value of 13.5 mg/kg i.p.
Animal Model: Wistar (male, 500 g, PCP-induced EEG power spectral change model)[4]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently attenuated PCP-induced power decrements at higher frequencies (5-30 Hz) in prefrontal and sensorimotor cortices.
Induced synchronization peaks at 3-5 Hz and 8-20 Hz frequency bands in the prefrontal cortex at 10 mg/kg i.p.
Animal Model: Wistar (male, 250-300 g, neuronal hypofunction induced by NMDA receptor glycineB site blockade)[5]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Reversed L-701324-induced inhibition of dorsal raphe nucleus neuron firing, restoring rates from 3.64 Hz to near control levels (7.64 vs. 7.92 Hz) with statistical significance.
Increased firing within 1 minute after injection, peaked at 4–5 minutes, then declined gradually.
Tended to elevate dorsal raphe nucleus neuronal firing when given alone, but the effect was not significant.
分子量

367.36

Formula

C19H20F3NO3
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

Org 24461 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

Org 24461372198-80-6Org24461Org-24461GlyTGlycine transportersrisperidoneblood-brain barrierschizophreniaCHO cells7-chlorokynurenic acidstriatal dopaminePCPGlyT-1glycineNMDA receptorsInhibitorinhibitorinhibit

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