TRPV1 antagonist 11 (compound 2ac) is a highly potent TRPV1 antagonist with an IC50 of 29.3 nM. It also acts as a µ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. This pyrimidinylpiperazine compound provides analgesic effects by antagonizing TRPV1 and activating MOR. In mouse models of formalin-induced pain, TRPV1 antagonist 11 demonstrates effective dose-dependent antinociceptive properties.
Formel:
C31H37N7O2
Target-Kategorie:
Opioid Receptor|||TRP/TRPV Channel
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