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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 1638667-81-8
- Formule: C22H25Cl2NO3
- Masse moléculaire:422.34
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform Dopamine Receptor
More
Activité biologique
|
Human D1 Receptor 5.8 nM (EC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
12 nM
Compound: 33; DETQ
|
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
|
[PMID: 30525590] |
| HEK293 | EC50 |
13.9 nM
Compound: 1; DETQ
|
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
|
[PMID: 31532644] |
| HEK293 | EC50 |
162 nM
Compound: 33; DETQ
|
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
|
[PMID: 30525590] |
| HEK293 | EC50 |
312 nM
Compound: 33; DETQ
|
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
|
[PMID: 30525590] |
| HEK293 | EC50 |
5.8 nM
Compound: 33; DETQ
|
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
|
[PMID: 30525590] |
| HEK293 | EC50 |
8.6 nM
Compound: 33; DETQ
|
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
|
[PMID: 30525590] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mice genetically modified to express the human D1 receptor ("hD1 mice")[2]
-
Dosage:10 mg/kg
-
Administration:i.p.; once
-
Result:Ameliorated subchronic Phencyclidine-induced object recognition memory deficits.
Chemical Information
-
CAS No. 1638667-81-8
-
Masse moléculaire 422.34
-
Formule C22H25Cl2NO3
-
SMILES
C[C@@H]1N(C(CC2=C(Cl)C=CC=C2Cl)=O)[C@@H](CO)CC3=C1C=CC=C3C(C)(O)C
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DETQ Related Classifications
HY-115553 Related Classifications
Powered by Bioz