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