TIK-301

TIK‑301 is a small molecule, orally active melatonergic drug that acts as a potent agonist at the melatonin MT1 and MT2 receptors, with high affinity (Ki values of 0.081 nM and 0.042 nM, respectively)[5][6]. It also functions as an antagonist at serotonin 5‑HT2B and 5‑HT2C receptors[3][5][6]. Originally developed by Eli Lilly, TIK‑301 has been investigated for the treatment of insomnia, circadian rhythm sleep disorders (including in totally blind individuals), depression, tardive dyskinesia in schizophrenia patients, and other conditions such as mild cognitive impairment[1][3]. The drug has demonstrated efficacy in reducing sleep latency and shifting circadian phase but does not improve sleep maintenance[1]. It was granted orphan drug designation by the FDA for circadian rhythm disorders in blind individuals and tardive dyskinesia[3][4].

Other names

Beta-methyl-6-chloromelatoninBeta-methyl6-chloromelatoninBeta-methyl 6-chloromelatonin(R)-N-[2-(6-Chloro-5-Methoxy-1H-Indol-3-Yl)Propyl]AcetamideN-(2r)-2-(6-chloro–5-methoxy–1h-indol–3–yl)propylacetamide