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MQ02-439

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MQ02-439
Clinical data
Other names1-Methoxynoraporphine; Compound 18b
Drug classSerotonin 5-HT2C receptor agonist
ATC code
  • None
Identifiers
  • 1-methoxy-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H17NO
Molar mass251.329 g·mol−1
3D model (JSmol)
  • COC1=C2C3=CC=CC=C3CC4C2=C(CCN4)C=C1
  • InChI=1S/C17H17NO/c1-19-15-7-6-11-8-9-18-14-10-12-4-2-3-5-13(12)17(15)16(11)14/h2-7,14,18H,8-10H2,1H3
  • Key:MHHVBPCYYCUVPT-UHFFFAOYSA-N

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 EC50Tooltip half-maximal effective concentration (EmaxTooltip maximal efficacy) 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

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References

[edit]
  1. ^ a b c d e f g h Mao Q, Zhang B, Li W, Tian S, Shui W, Ye N (February 2020). "Identification of Novel 1-O-Substituted Aporphine Analogues as Potent 5-HT2C Receptor Agonists". ACS Chemical Neuroscience. 11 (4): 549–559. doi:10.1021/acschemneuro.9b00563. PMID 31968160.
  2. ^ Mao Q, Zhang B, Tian S, Qin W, Chen J, Huang XP, et al. (June 2022). "Structural optimizations and bioevaluation of N-H aporphine analogues as Gq-biased and selective serotonin 5-HT2C receptor agonists". Bioorganic Chemistry. 123 105795. doi:10.1016/j.bioorg.2022.105795. PMID 35430417.
  3. ^ Qin W, Zhang B, Wang Q, Jiang G, Cui J, Chen F, et al. (November 2025). "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. doi:10.1021/acs.jmedchem.5c02115. PMID 41108743.
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