2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. NGD 94-1 dimaleate

NGD 94-1 (dimaleate) 是一种强效且选择性的多巴胺 D4 受体 (dopamine D4 receptor) 拮抗剂。NGD 94-1 (dimaleate) 对克隆人源 D4.2 受体 (human D4.2 receptor) 具有高亲和力 (Ki = 3.6 nM)。NGD 94-1 (dimaleate) 在 Phencyclidine (PCP) 诱导的猴子模型中可调节前额叶-纹状体系统的认知功能，并调控多巴胺能神经传递。NGD 94-1 (dimaleate) 可用于神经系统疾病的相关研究[1][2]。

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NGD 94-1 dimaleate

NGD 94-1 dimaleate Chemical Structure

CAS No. : 179333-18-7

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NGD 94-1 dimaleate 相关抗体

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  • 生物活性

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生物活性

NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research[1][2].

IC50 & Target[2]

hD4.2 Receptor

3.6 nM (Ki)

体外研究
(In Vitro)

NGD 94-1 (dimaleate) 对 D4.2 受体的选择性比其他许多靶点高 600 倍以上，然而，其对 5-HT1A 受体 (选择性低约 50 倍) 和 5-HT3 受体 (选择性低约 200 倍) 的选择性则显著较低[2]。
NGD 94-1 (dimaleate) 在 HEK293/D4 细胞中可诱导 cAMP 积累的抑制，但在未转染的 HEK293 细胞中不影响 Forskolin (HY-15371) 刺激的 cAMP 生成，表明其抑制作用是通过转染的多巴胺 D4 受体特异性介导[3]。

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

NGD 94-1 dimaleate 相关抗体:
体内研究
(In Vivo)

NGD 94-1 (1-5 mg/kg，肌肉注射，测试前 45 分钟给药) (dimaleate) 可逆转 PCP 预处理猴子的认知缺陷，并增加脑池脑脊液中 HVA 的积累[1]。

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

Animal Model: Young-adult vervet (Cercopithecus aethiops sabaeus) monkeys[1]
Dosage: 1 and 5 mg/kg
Administration: i.m., 45 min prior to testing
Result: Significantly reversed the impaired successful performance of PCP-treated subjects (from 58% to 79% accuracy) at 1 mg/kg.
Ameliorated the PCP-induced impairments (from 73% to 86% accuracy) at 5 mg/kg.
Reduced barrier reaching and perseverative responding at both doses in PCP-treated monkeys.
Unaffected response initiation latencies and motor problems in PCP-treated monkeys.
Unaffected accurate performance at 1 mg/kg in saline pretreated monkeys.
Slightly impaired successful performance at 5 mg/kg in saline pretreated monkeys.
Failed to affect response initiation latencies or motor problems at both doses in saline pretreated monkeys.
Failed to affect HVA levels relative to saline in control subjects.
Significantly increased HVA concentrations in the CSF in PCP-treated subjects.
分子量

552.54

Formula

C26H28N6O8
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

NGD 94-1 dimaleate 相关分类

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Keywords:

NGD 94-1 dimaleate179333-18-7Dopamine Receptordopamine D4 receptorhuman D4.2 receptorfrontostriatalPhencyclidinevervet monkeyInhibitorinhibitorinhibit

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