TIK-301

Names

[ Name ]:
TIK-301

[Synonym ]:
N-[(2R)-2-(6-Chloro-5-methoxy-1H-indol-3-yl)propyl]acetamide
Acetamide, N-[(2R)-2-(6-chloro-5-methoxy-1H-indol-3-yl)propyl]-
LY-156,735
PD-6735
3ZX95B1ZWK
TIK-301

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Melatonin Receptor

Signaling Pathways >> GPCR/G Protein >> Melatonin Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

melatonin MT1:0.081 nM (Ki)

melatonin MT2:0.042 nM (Ki)

5-HT2C Receptor

5-HT2B Receptor

[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].

[References]

[1]. Paulis L, et al. Cardiovascular effects of melatonin receptor agonists. Expert Opin Investig Drugs. 2012 Nov;21(11):1661-78.

[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.

[3]. Carocci A, et al. Melatonergic drugs in development. Clin Pharmacol. 2014 Sep 18;6:127-37.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
525.9±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₇ClN₂O₂

[ Molecular Weight ]:
280.750

[ Flash Point ]:
271.9±30.1 °C

[ Exact Mass ]:
280.097870

[ LogP ]:
1.86

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.596

Related Compounds

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