Luzindole
Cat. No.:YN320118
产品名称: | Luzindole |
CAS No.: | 117946-91-5 |
Chemical Name: | N-[2-[2-(phenylmethyl)-1H-indol-3-yl]ethyl]-acetamide |
Synonyms: | N-0774 |
分子量: | 292.37 |
分子式: | C₁₉H₂₀N₂O |
SMILES: | CC(NCCC1=C(CC2=CC=CC=C2)NC3=C1C=CC=C3)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Luzindole (N-0774) 是一种选择性褪黑素受体 (melatonin receptor) 拮抗剂。Luzindole 优先靶向 MT2 (Mel1b),对于人 MT2 和 MT1 的Ki值分别为 10.2 和 158 nM。Luzindole 抑制实验性自身免疫性脑脊髓炎,并发挥抗抑郁样活性。 |
IC50和靶点: | |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Chan, K.H., and Wong, Y.H.A molecular and chemical perspective in defining melatonin receptor subtype selectivityInt. J. Mol. Sci.14(9),18385-18406(2013)
Teh, M.T., and Sugden, D.Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: Lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophoresNaunyn Schmiedebergs Arch. Pharmacol.358(5),522-528(1998)
Dubocovich, M.L.Luzindole (N-0774): A novel melatonin receptor antagonistJ. Pharmacol. Exp. Ther.246(3),902-910(1988)
Dubocovich, M.L., Masana, M.I., Iacob, S., et al.Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptorNaunyn-Schmiedeberg's Arch. Pharmacol.355(3),365-375(1997)
Dubocovich, M.L., Yun, K., Al-Ghoul, W.M., et al.Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythmsFASEB J.12(12),1211-1220(1998)
Laredo, S.A., Orr, V.N., McMackin, M.Z., et al.The effects of exogenous melatonin and melatonin receptor blockade on aggression and estrogen-dependent gene expression in male California mice (Peromyscus californicus)Physiol. Behav.128,86-91(2014)