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TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment[1][2][3]. | [in vivo]
In male rats, TIK-301(at doses of 0.8 and 4.0 mg/kg/day) can reduce body weight, and without altering food intake[1][2].
The Tmax and half-life of TIK-301 is 1.1 hour and 1 hour, respectively[1]. | [IC 50]
melatonin MT1: 0.081 nM (Ki); melatonin MT2: 0.042 nM (Ki); 5-HT2C Receptor; 5-HT2B Receptor | [References]
[1] Paulis L, et al. Cardiovascular effects of melatonin receptor agonists. Expert Opin Investig Drugs. 2012 Nov;21(11):1661-78. DOI:10.1517/13543784.2012.714771
[2] Rivara S, et al. Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders. Curr Top Med Chem. 2008;8(11):954-68. DOI:10.2174/156802608784936719
[3] Carocci A, et al. Melatonergic drugs in development. Clin Pharmacol. 2014 Sep 18;6:127-37. DOI:10.2147/CPAA.S36600 |
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