The KOR is widely expressed in several areas of CNS and large body of evidence (both human and rodents studies) during last 4 decades have showed that antagonist of this receptor suppress the anxiety and ameliorates depression like symptoms in mice models. Furthermore, several KOR antagonists are currently in advance stage of clinical trials, testifying aforementioned findings. Thus, obtaining a novel KOR antagonist with drug like properties can be developed as first in class drug for the treatment of depression. Moreover, results of ongoing clinical trials have shown that this class of drugs are effective in treatment resistant depressed patients
S013-1304 is not completely a novel chemical entity, but is a selective and potent KOR antagonist with pIC50<-5.5 .This compound also acts as a agonist of TrkB receptor (anther target of Depression). S013-1304 (10 mg/kg) reversed the depression like symptoms in CUS model of depression and effect is comparable to Fluoxetine, a widely prescribed antidepressant drug. Furthermore, S013-1304 does not bind to hERG ion channel up to 10 µM.
This compound hits two very popular and well established target of depression, and therefore it produces very robust efficacy in vivo models of depression despite of modest affinity at one target..
The S013-1304 could be developed as first in class candidate drug for refractory depression, for which no drug is approved, yet.
Patent for new use is yet to be filed.