| Identification | Back Directory | [Name]
2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethy l)-5-(2-hydroxypropan-2-yl)-1-methyl-1,2,3,4-tetrah ydroisoquinolin-2-yl]ethan-1-one | [CAS]
1638667-81-8 | [Synonyms]
Ethanone, 2-(2,6-dichlorophenyl)-1-[(1S,3R)-3,4-dihydro-3-(hydroxymethyl)-5-(1-hydroxy-1-methylethyl)-1-methyl-2(1H)-isoquinolinyl]-
2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethy l)-5-(2-hydroxypropan-2-yl)-1-methyl-1,2,3,4-tetrah ydroisoquinolin-2-yl]ethan-1-one | [Molecular Formula]
C22H25Cl2NO3 | [MOL File]
1638667-81-8.mol | [Molecular Weight]
422.34 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
DETQ (10 mg/kg; i.p.; once) ameliorates subchronic Phencyclidine-induced object recognition memory deficits and enhances cortical acetylcholine efflux in male humanized D1 receptor knock-in mice[2]. | 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.
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| [IC 50]
Human D1 Receptor: 5.8 nM (EC50) | [References]
[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. DOI:10.1124/jpet.116.236372
[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. DOI:10.1016/j.bbr.2018.12.006 |
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