118702-11-7

118702-11-7 structure

Name: TIK-301
Chemical Name: LY-156,735
CAS Number: 118702-11-7
Molecular Formula: C₁₄H₁₇ClN₂O₂
Molecular Weight: 280.750
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-07-15 03:04:15
Modify Date: 2024-01-02 17:14:13
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].

Name	LY-156,735
Synonyms	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

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.