Biochem/physiol Actions
β-arrestin-biased 5-HT7-selective agonist with antagonist/inverse agonist activity against Gs signaling and in vivo antinociceptive efficacy in mouse pain models.
Serodolin is a β-arrestin-biased, 5-HT7-selective 5-hydroxytryptamine receptor agonist (5HT7/2A/1A/6 Ki = 6.2/19/454/1224 nM) that induces ERK activation through a β-arrestin-dependent signaling mechanism that requires c-SRC activation (309% of basal pErk in 5HT7-transfected HEK293 post 2-15 min 10 μM treatment) while acting as an antagonist/inverse agonist against Gs signaling (IC50 = 14 & 5 nM, respectively, against basal and 10 nM 5-CT-induced cAMP production in 5HT7-transfected HEK293). Serodolin exhibits antinociceptive efficacy in response to inflammatory, thermal, and mechanical stimulation in mice in vivo (0.1-10 mg/kg s.c.).