180304-07-8

180304-07-8 structure

Name: S-22153
Chemical Name: N-[2-(5-Ethyl-1-benzothiophen-3-yl)ethyl]acetamide
CAS Number: 180304-07-8
Molecular Formula: C₁₄H₁₇NOS
Molecular Weight: 247.35600
Catalog: Signaling Pathways GPCR/G Protein Melatonin Receptor
Create Date: 2016-05-29 21:34:49
Modify Date: 2024-01-03 17:48:16
S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes[1][2].

Name	N-[2-(5-Ethyl-1-benzothiophen-3-yl)ethyl]acetamide

Description	S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes[1][2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Melatonin Receptor Signaling Pathways >> GPCR/G Protein >> Melatonin Receptor Research Areas >> Neurological Disease
Target	MT1:19 nM (EC50) MT2:4.6 nM (EC50)
In Vivo	S-22153 sets the temperature and activity periods to approximately 24 hr and increase the circadian amplitude of both rhythms in mice, which exposed to continuous light[1] . Animal Model: 7 weeks old Male B6D2F1 mice, which exposed to continuous light for 10-18 days[1] Dosage: 20 mg/kg Administration: Daily intraperitoneal (i.p.) for 19 days Result: Set the temperature and activity periods to approximately 24 hr and increased the circadian amplitude of both rhythms in mice, which exposed to continuous light.
References	[1]. Li XM, et al. Circadian rhythm entrainment with melatonin, melatonin receptor antagonist S22153 or their combination in mice exposed to constant light. J Pineal Res. 2004;37(3):176-184. [2]. Audinot V, et al. New selective ligands of human cloned melatonin MT1 and MT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003;367(6):553-561.