Z8779877149 (also known as A1CIZ, Z7149 or just '7149) is an indole derivative which acts at multiple targets, being a potent and selective serotonin reuptake inhibitor (SSRI), an agonist of the α2A adrenergic receptor, and a 5-HT2A receptor agonist. It was developed through an ultra-large-scale docking screen looking for compounds which would bind simultaneously at multiple targets, with the aim being to find compounds which would show both SSRI and α2A agonist activity, but off-target screening subsequently showed that it also acts as a 5-HT2A receptor agonist with similar potency. It has a binding affinity of 198 nM at the serotonin transporter (SERT) and 180 nM at α2A, with an EC50 of 170 nM at α2A and an EC50 of 172 nM at the 5-HT2A receptor, and an efficacy of 76% at 5-HT2A making it a partial agonist. In animal studies, '7149 showed results consistent with antidepressant, anxiolytic and analgesic effects thought to result from a combination of activity at all three targets.
See also (R)-69 Z3517967757 Z8526711350 ZINC000443438219
References


