ASP5633 is potent, highly selective peripherally restricted melatonin MT1/MT2 receptor agonist with EC50 of 12.3, 18.6, 36.2 and 36.4 nM for human MT1, human MT2, rat MT1 and rat MT2 by Ca2+ flux assays.
ASP5633 shows agonistic effects in human and rat MT1 and MT2 receptors without significant species differences in the assay using a Gqi chimeric protein to convert Gi signaling into intracellular Ca2+ responses.
ASP5633 shows no activity against a total of 56 receptors, ion channels, transporters and enzymes.
ASP5633 induced contraction of isolated rat urethral strips in a concentration-dependent manner (EC50=72 nM) in rat urethral strips, shows agonistic activity in MT1 receptor-mediated Gq signaling pathway.
ASP5633 (0.03–0.3 mg/kg) dose-dependently increased UPP with statistical significance at doses of 0.1 mg/kg in anesthetized rats.
ASP5633 increased urethral pressure in the bladder filling phase without affecting bladder pressure in either phase, or urethral pressure in the voiding phase.