DETQ

Potent and selective dopamine D₁ receptor positive allosteric modulator (K_b = 11.4nM and EC₅₀ = 5.8nM in human D₁ receptors). Suitable for use with genetically encoded dopamine sensors to enhance their 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 K_b of 54nM. Due to a 30-fold lower affinity for rodent D₁ receptors (Mouse D₁: K_b = 312nM) compared to human (K_b = 11.4), DETQ is suitable for chemogenetic modulation of human based dopamine sensors in rodents. No cross-reactivity observed with D₂, D₅, β2, 5HT₆ receptors. DETQ reverses reserpine induced locomotor deficits alongside increasing PFC histamine and acetylcholine concentrations in human D1 expressing mice. Orally bioavailable, active in-vivo and blood brain barrier permeable.

Soluble in DMSO

-20°C

For in vivo administration, Labouesse MA et al (2024) use a vehicle consisting of 20% 2-hydroxy-propyl-beta-cyclodextrin in puriified water with ultrasonication

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

C₂₂H₂₅Cl₂NO₃