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DETQ 

Cat. No. M28748
DETQ  Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 422.34
Formula C22H25Cl2NO3
CAS Number 1638667-81-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kjell A Svensson, et al. Adv Pharmacol. Positive allosteric modulators of the dopamine D1 receptor: A new mechanism for the treatment of neuropsychiatric disorders

[2] Herbert Y Meltzer, et al. Behav Brain Res. 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

[3] Xushan Wang, et al. Mol Pharmacol. Intracellular Binding Site for a Positive Allosteric Modulator of the Dopamine D1 Receptor

[4] Robert F Bruns, et al. Neuropharmacology. Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders

[5] Kjell A Svensson, et al. J Pharmacol Exp Ther. An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis

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Keywords: DETQ  supplier, Dopamine Receptor, inhibitors, activators

 
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