美国麻薩諸塞州东北大学亚历山德罗斯·马克里扬尼斯(Alexandros Makriyannis)的研究小组合成了许多大麻素,统称为AM大麻素,其中一些是:
大麻素及其Ki值(Ki是化合物对大麻素1型受体(CB1)或大麻素2型受体(CB2)的结合亲和力) 名称 | 类别 | 分子式 | Ki/nM (CB1) | Ki/nM (CB2) | 选择性 | 结构 | ref |
AM-087 | 二苯并吡喃 | C23H33BrO2 | 0.43 | | | | |
AM-251 | 吡唑衍生物 | C22H21Cl2IN4O | 7.5 | | | | [1] |
AM-356 | | C23H39NO2 | 17.9 | 868 | | | [2] |
AM-404 | | C26H37NO2 | | | | | |
AM-411 | 二苯并吡喃 | C26H34O2 | 6.8 | 52.0 | | | |
AM-630 | 苯甲酰基吲哚 | C23H25IN2O3 | | 32.1 | CB2(165×) | | |
AM-678 | 萘甲酰基吲哚 | C24H23NO | 9.00±5.00 | 2.94±2.65 | CB2 | | |
AM-679 | 苯甲酰基吲哚 | C20H20INO | 13.5 | 49.5 | CB1 | | |
AM-694 | 苯甲酰基吲哚 | C20H19FINO | 0.08 | 1.44 | CB1(18×) | | [3] |
AM-855 | | C26H38O2 | 22.3 | 58.6 | CB1 | | |
AM-905 | | C23H34O3 | 1.2 | 5.3 | CB1 | | |
AM-906 | | C23H34O3 | 0.8 | 9.5 | CB1 | | |
AM-919 | | C27H44O4 | 2.2 | 3.4 | CB1 | | |
AM-938 | | C27H40O4 | 1.2 | 0.3 | CB2(4×) | | |
AM-1220 | 萘甲酰基吲哚 | C26H26N2O | 3.88 | 73.4 | CB1 (19×) | | [4][5] |
AMG系列大麻素 名称 | 类别 | 分子式 | 结构 | CAS号 |
AMG-1 | 二苯并吡喃 | C23H30O2 | | 205746-46-9 |
AMG-3 | 二苯并吡喃 | C25H36O2S2 | | 179044-94-1 |
AMG-36 | 二苯并吡喃 | C27H40O2 | | 579444-43-2 |
AMG-41 | 二苯并吡喃 | C25H36O2 | | 499237-35-3 |
参见
- CP大麻素列表
- HU大麻素列表
- JWH大麻素列表
- 杂项设计师大麻素列表(英语:List of miscellaneous designer cannabinoids)
参考文献
- ^ Lan, Ruoxi; Lu, Qian; Fan, Pusheng; Gatley, John; Volkow, Nora D.; Fernando, Susanthi R.; Pertwee, Roger; Makriyannis, Alexandros. Design and synthesis of the CB1 selective cannabinoid antagonist AM281: A potential human SPECT ligand. AAPS PharmSci. 1999, 1 (2): 39–45. PMC 2761119 . PMID 11741201. doi:10.1208/ps010204.
- ^ Selwood, D. The Cannabinoid Receptors. Edited by Patricia H. Reggio. ChemMedChem. 2009, 4: 1949. doi:10.1002/cmdc.200900286.
- ^ Template:Ref patent2
- ^ D'ambra, T. C-Attached aminoalkylindoles: potent cannabinoid mimetics. Bioorganic & Medicinal Chemistry Letters. 1996, 6: 17–22. doi:10.1016/0960-894X(95)00560-G.
- ^ Willis, P. G.; Pavlova, O. A.; Chefer, S. I.; Vaupel, D. B.; Mukhin, A. G.; Horti, A. G. Synthesis and Structure−Activity Relationship of a Novel Series of Aminoalkylindoles with Potential for Imaging the Neuronal Cannabinoid Receptor by Positron Emission Tomography. Journal of Medicinal Chemistry. 2005, 48 (18): 5813–22. PMID 16134948. doi:10.1021/jm0502743.