DETQ

Last updated

DETQ
DETQ structure.png
Identifiers
  • 2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethyl)-5-(2-hydroxypropan-2-yl)-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl]ethanone
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C22H25Cl2NO3
Molar mass 422.35 g·mol−1
3D model (JSmol)
  • C[C@H]1C2=C(C[C@@H](N1C(=O)CC3=C(C=CC=C3Cl)Cl)CO)C(=CC=C2)C(C)(C)O
  • 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
  • Key:CWRORBWPLQQFMX-UONOGXRCSA-N

DETQ is an experimental drug which acts as a positive allosteric modulator of the Dopamine receptor D1. It increases the D1-mediated response to endogenous dopamine levels, and was developed as a potential treatment for Parkinson's disease. [1] [2] [3] [4] [5]

See also

References

  1. ↑ Svensson KA, Heinz BA, Schaus JM, Beck JP, Hao J, Krushinski JH, et al. (January 2017). "An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis". The Journal of Pharmacology and Experimental Therapeutics. 360 (1): 117–128. doi:10.1124/jpet.116.236372. PMC   5193077 . PMID   27811173.
  2. ↑ Bruns RF, Mitchell SN, Wafford KA, Harper AJ, Shanks EA, Carter G, et al. (January 2018). "Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders". Neuropharmacology. 128: 351–365. doi: 10.1016/j.neuropharm.2017.10.032 . PMID   29102759.
  3. ↑ Svensson KA, Hao J, Bruns RF (2019). "Positive allosteric modulators of the dopamine D1 receptor: A new mechanism for the treatment of neuropsychiatric disorders". Neuropsychotherapeutics. Advances in Pharmacology. Vol. 86. San Diego, Calif.: Elsevier. pp. 273–305. doi:10.1016/bs.apha.2019.06.001. ISBN   978-0-12-816668-0. PMID   31378255.
  4. ↑ Meltzer HY, Rajagopal L, Matrisciano F, Hao J, Svensson KA, Huang M (April 2019). "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". Behavioural Brain Research. 361: 139–150. doi:10.1016/j.bbr.2018.12.006. PMID   30521930.
  5. ↑ Rajagopal L, Huang M, Mahjour S, Ryan C, Elzokaky A, Svensson KA, et al. (February 2024). "The dopamine D1 receptor positive allosteric modulator, DETQ, improves cognition and social interaction in aged mice and enhances cortical and hippocampal acetylcholine efflux". Behavioural Brain Research. 459 114766. doi:10.1016/j.bbr.2023.114766. PMID   38048913.
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