Chemistry:MQ02-439

From HandWiki

MQ02-439, also known as 1-methoxynoraporphine, is a serotonin 5-HT2C receptor agonist of the noraporphine family.[1] It is a potent and selective full agonist of the serotonin 5-HT2C receptor, with an EC50 (Emax) of 103 nM (96%).[1] The drug showed no activation of the serotonin 5-HT2A and 5-HT2C receptors at concentrations of up to 10,000 nM.[1] However, it did show weak antagonism of these two receptors.[1] The chemical synthesis of MQ02-439 has been described.[1] Various analogues of MQ02-439 have also been described, including some with potent serotonin 5-HT2A receptor agonist activity.[1][2][3] The (S)- enantiomer of MQ02-439 is known as MQ02-592 and is the more potent enantiomer in terms of serotonin 5-HT2C receptor agonism.[1] MQ02-439 was described in the scientific literature by Qi Mao and colleagues in 2020.[1]

See also

  • Noraporphine
  • 11-Chloroasimilobine
  • 2-Hydroxy-11-(2-methylallyl)oxynoraporphine
  • Nornuciferine
  • Asimilobine
  • 11-Methoxyasimilobine

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 "Identification of Novel 1-O-Substituted Aporphine Analogues as Potent 5-HT2C Receptor Agonists". ACS Chemical Neuroscience 11 (4): 549–559. February 2020. doi:10.1021/acschemneuro.9b00563. PMID 31968160. 
  2. ↑ "Structural optimizations and bioevaluation of N-H aporphine analogues as Gq-biased and selective serotonin 5-HT2C receptor agonists". Bioorganic Chemistry 123. June 2022. doi:10.1016/j.bioorg.2022.105795. PMID 35430417. 
  3. ↑ "Discovery of New N-H Aporphine Derivatives As Brain-Penetrant Gq-Biased 5-HT2C Receptor Agonists and Dual 5-HT2C/5-HT2A Receptor Agonists". Journal of Medicinal Chemistry 68 (21): 23300–23323. November 2025. doi:10.1021/acs.jmedchem.5c02115. PMID 41108743. 



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