Product overview

Name DETQ
Description

Dopamine D1 receptor selective allosteric potentiator, enhances genetically encoded dopamine sensor sensitivity.

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Biological Data

Biological description

Potent and selective dopamine D1 receptor positive allosteric modulator (Kb = 11.4nM and EC50 = 5.8nM in human D1 receptors) suitable for use with genetically encoded dopamine sensors to enhance sensitivity. When used with the dLight1.3b genetically encoded dopamine sensor, DETQ administration leads to an 8-fold increase in dopamine sensitivity (2µM to 244nM) with a Kb of 54nM. Due to a 30-fold lower affinity for rodent D1 receptors (Mouse D1: Kb = 312nM) compared to human (Kb = 11.4) this makes DETQ suitable for chemogenetic modulation of human based dopamine sensors in rodents. No cross-reactivity observed with D2, D5, β2, 5HT6 receptors. Orally bioavailable and active in-vivo. DETQ reverses reserpine induced locomotor deficits alongside increasing PFC histamine and acetylcholine concentrations in human D1 expressing mice.

Solubility & Handling

Storage instructions

-20°C

Solubility overview

Soluble in DMSO, 20% hydroxypropylbetacyclodextrin (3mg/ml) and 1% hydroxyethylcellulose (2mg/ml)

Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

Molarity

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Dilution

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Chemical Data

Chemical name

2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethyl)-5-(2-hydroxypropan-2-yl)-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl]ethanone

Molecular Weight 422.3
Chemical structure DETQ chemical structure Chemical Structure
Molecular Formula C22H25Cl2NO3
CAS Number 1638667-81-8
PubChem identifier 117720272
SMILES C[C@H]1C2=C(C[C@@H](N1C(=O)CC3=C(C=CC=C3Cl)Cl)CO)C(=CC=C2)C(C)(C)O
Source Synthetic
InChi InChI=1S/C22H25Cl2NO3/c1-13-15-6-4-7-18(22(2,3)28)16(15)10-14(12-26)25(13)21(27)11-17-19(23)8-5-9-20(17)24/h4-9,13-14,26,28H,10-12H2,1-3H3/t13-,14+/m0/s1
InChiKey CWRORBWPLQQFMX-UONOGXRCSA-N

References for DETQ

References are publications that support the biological activity of the product
  • A chemogenetic approach for dopamine imaging with tunable sensitivity

    Labouesse MA et al (2024) Nature Communications :
  • Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders

    Bruns RF et al (2018) Neuropharmacology :
  • Intracellular Binding Site for a Positive Allosteric Modulator of the Dopamine D1 Receptor

    Wang X et al (2018) Molecular Pharmacology :

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