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Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists

Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists

  1. Anonymous
    Lange JH, Attali A, van der Neut MA, Wals HC, Mulder A, Zilaout H, Duursma A, van Aken, HH, van Vliet, BJ Bioorg Med Chem Lett.2010 Sep 1;20(17):4992-8. Epub 2010 Jul 17. PMID: 20688519

    The synthesis and SAR of 3-alkyl-4-aryl-4,5-dihydropyrazole-1-carboxamides 1–23 and 1-alkyl-5-aryl-
    4,5-dihydropyrazole-3-carboxamides 24–27 as two novel cannabinoid CB1 receptor agonist classes were
    described. The target compounds elicited high affinities to the CB1 as well as the CB2 receptor and were found to act as CB1 receptor agonists. The key compound 19 elicited potent CB1 agonistic and CB2 inverse agonistic properties in vitro and showed in vivo activity in a rodent model for multiple sclerosis after oral administration.