LE 300
Cat. No.:YN1730145
产品名称: | LE 300 |
CAS No.: | 274694-98-3 |
Chemical Name: | 6,7,8,9,14,15-hexahydro-7-methyl-5H-indolo[3,2-f][3]benzazecine |
Synonyms: | |
分子量: | 290.40216 |
分子式: | C20H22N2 |
SMILES: | CN1CCC2=C(CC3=C(C=CC=C3)CC1)NC4=C2C=CC=C4 |
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: | LE 300 是一种有效的选择性多巴胺 D1 样受体拮抗剂,在表达人多巴胺 D1 和 D5 受体的 CHO 细胞膜中,其Kis 分别为 1.9 nM 和 7.5 nM。在一项大鼠尾动脉实验中,LE 300 是5-HT2A受体的拮抗剂,pA2 为 8.32。 |
IC50和靶点: | [{name:"Human D1 Receptor:1.9 nM (Ki)"},{name: "Human D5 Receptor:7.5 nM (Ki)"},{name: "Rat 5-HT2A:8.32 (pA2)"}] |
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Clinical Trial: | |
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Kassack, M.U., Höfgen, B., Decker, M., et al.Pharmacological characterization of the benz[d]indolo[2,3-g]azecine LE300, a novel type of a nanomolar dopamine receptor antagonistNaunyn Schmiedebergs Arch. Pharmacol.366(6),543-550(2002)
Rostom, S.A.F.Novel fused pyrrole heterocyclic ring systems as structure analogs of LE 300: Synthesis and pharmacological evaluation as serotonin 5-HT2A, dopamine and histamine H1 receptor ligandsArch. Pharm. Chem. Life Sci.343(2),73-80(2010)
Schulze, M., Siol, O., Robaa, D., et al.Molecular combination of the dopamine and serotonin scaffolds yield in novel antipsychotic drug candidates - characterization by in vivo experimentsArzneimittelforschung62(5),252-260(2012)