VU0466551 was recently tested in vivo as a potential supplement to opioid analgesics in a mouse pain model [31, 32]. Abney and collaborators examined the potential analgesic efficacy of VU0466551 [31]. In two murine models of nociception, a 30 mg/kg injection of VU0466551 produced analgesic efficacy, either alone (formalin test) or in combination with sub-maximally effective doses of morphine (formalin and hotplate tests), enhancing the analgesia exerted by the opioid (Figure 3). Despite the weak off-target effect of VU0466551 on NaV1.7 channels [31], these findings highlight GIRK activation as a potential therapeutic approach for analgesia.
