ADRIANA is potent antagonist (IC50 = 1.71 µM) of the alpha2B adrenoceptor with selectivity over alpha2A and alpha2C. It promotes noradrenaline release in the murine spinal dorsal horn leading to potent analgesic effects via stimulation of the alpha2A-dependent pain inhibitory pathway. Active in various nociceptive pain models in both mice and non-human primates. Orally bioavailable with no adverse cardiac/circulatory system effects.
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