DETQ
DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1638667-81-8
- 分子式: C22H25Cl2NO3
- 分子量:422.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Dopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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Human D1 Receptor 5.8 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
12 nM
Compound: 33; DETQ
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Positive allosteric modulation of rhesus monkey D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
Positive allosteric modulation of rhesus monkey D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
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[PMID: 30525590] |
| HEK293 | EC50 |
13.9 nM
Compound: 1; DETQ
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Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
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[PMID: 31532644] |
| HEK293 | EC50 |
162 nM
Compound: 33; DETQ
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Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
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[PMID: 30525590] |
| HEK293 | EC50 |
312 nM
Compound: 33; DETQ
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Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
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[PMID: 30525590] |
| HEK293 | EC50 |
5.8 nM
Compound: 33; DETQ
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Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
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[PMID: 30525590] |
| HEK293 | EC50 |
8.6 nM
Compound: 33; DETQ
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Positive allosteric modulation of dog D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
Positive allosteric modulation of dog D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
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[PMID: 30525590] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice genetically modified to express the human D1 receptor ("hD1 mice")[2]
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Dosage:10 mg/kg
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Administration:i.p.; once
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Result:Ameliorated subchronic Phencyclidine-induced object recognition memory deficits.
化学情報
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CAS 番号 1638667-81-8
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分子量 422.34
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分子式 C22H25Cl2NO3
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SMILES
C[C@@H]1N(C(CC2=C(Cl)C=CC=C2Cl)=O)[C@@H](CO)CC3=C1C=CC=C3C(C)(O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Kjell A Svensson, et al. An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis. J Pharmacol Exp Ther. 2017 Jan;360(1):117-128. [Content Brief]
[2]. Herbert Y Meltzer, et al. The allosteric dopamine D1 receptor potentiator, DETQ, ameliorates subchronic phencyclidine-induced object recognition memory deficits and enhances cortical acetylcholine efflux in male humanized D1 receptor knock-in mice. Behav Brain Res. 2019 Apr 1;361:139-150. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
DETQ 関連分類
HY-115553 関連分類
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