PZKKN-94

PZKKN-94
Clinical data
Other namesPZKKN94
Drug classSerotonin; 5-HT1B receptor agonist; Serotonin 5-HT6 receptor antagonist; Antiparkinsonian agent
ATC code
  • None
Identifiers
  • 2-(2,4-difluorophenyl)sulfonyl-4-piperazin-1-yl-1,3-dihydroisoindole
PubChem CID
Chemical and physical data
FormulaC18H19F2N3O2S
Molar mass379.43 g·mol−1
3D model (JSmol)
  • C1CN(CCN1)C2=CC=CC3=C2CN(C3)S(=O)(=O)C4=C(C=C(C=C4)F)F
  • InChI=1S/C18H19F2N3O2S/c19-14-4-5-18(16(20)10-14)26(24,25)23-11-13-2-1-3-17(15(13)12-23)22-8-6-21-7-9-22/h1-5,10,21H,6-9,11-12H2
  • Key:PMKDLPXTADKLHI-UHFFFAOYSA-N

PZKKN-94 is a dual serotonin 5-HT1B receptor agonist and serotonin 5-HT6 receptor antagonist which is under investigation for the potential treatment of Parkinson's disease.[1] Its values were 39 nM (EC50Tooltip half-maximal effective concentration) and 88.1% (EmaxTooltip maximal efficacy) at the serotonin 5-HT1B receptor and 7.7 nM (KB) at the serotonin 5-HT6 receptor.[1] The drug showed selectivity for these receptors over 43 other targets.[1] It shows favorable drug-like properties.[1] In rodents, PZKKN-94 shows antiparkinsonian-like, pro-cognitive, and antidepressant-like effects.[1] PZKNN-94 was first described in the scientific literature by Paweł Zajdel and colleagues in 2025.[1]

See also

References

  1. ^ a b c d e f Zajdel P, Matłoka M, Konieczny J, Kos T, Lammers JC, Cavalco NG, et al. (February 2025). "Simultaneous 5-HT1BR agonist/5-HT6R antagonist action as a potential treatment of Parkinson's disease and its comorbidities". The Journal of Pharmacology and Experimental Therapeutics. 392 (2) 100055. doi:10.1016/j.jpet.2024.100055. PMID 40023605.
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