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Submit ReviewML 154 is a potent neuropeptide S receptor (NPSR) antagonist (pA2 = 9.98). Inhibits neuropeptide S-induced ERK phosphorylation over cAMP responses and calcium responses (IC50 values are 9.3, 22.1 and 36.5 nM, respectively). Appears to modulate addictive behavior in vivo. Displays no activity against vasopressin V1B receptors. Brain penetrant.
分子量 | 545.47 |
公式 | C29H26N2PS.Br |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 1345964-89-7 |
PubChem ID | 46930969 |
InChI Key | CJAQCMBWGUOBIX-ZUQRMPMESA-M |
Smiles | CC1=C(P(C4=CC=CC=C4)(C5=CC=CC=C5)=S)N3C(C=CC=C3)=[N+]1C/C=C/C2=CC=CC=C2.[Br-] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Patnaik et al (2013) Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor. J Med Chem. 56 9045 PMID: 24171469
Thorsell et al (2013) A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant alcohol self-administration in rats. J.Neurosci. 33 10132 PMID: 23761908
关键词: ML 154, ML 154 supplier, ML154, Potent, selective, Neuropeptide, S, receptors, NPSR, antagonists, ERK, phosphorylation, additive, behaviour, Blood, brain, barrier, permeable, Receptors, 5161, Tocris Bioscience
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