凡能够模拟乙酰胆碱作用的药物统称为拟胆碱药。根据其作用原理不同,这类药物可分为胆碱受体激动药和胆碱酯酶抑制药两大类。
胆碱受体激动药能直接与胆碱受体结合,产生类似乙酰胆碱的效果。而乙酰胆碱作为胆碱能神经递质,能够激活M型和N型胆碱受体。
具体来说,当M受体被激活时,会表现出心脏抑制、血管扩张、内脏平滑肌收缩、括约肌松弛以及腺体分泌增加等症状,这些效应被称为“M样作用”。而当N受体被激活时,则会引起神经节兴奋和骨骼肌收缩,这称为“N样作用”。
由于乙酰胆碱化学性质不稳定,在体内很快被胆碱酯酶水解失效,并且其作用范围广泛、选择性不高,因此在临床上并无实际应用价值。然而,某些与乙酰胆碱结构相似的化合物,虽然较为稳定且具有较高的选择性,却具备一定的临床用途。
| 中文名称 | 英文名称 | CAS号 | 化学式 |
|---|---|---|---|
| 酒石酸氢胆碱 | choline (R,R)-hydrogentartrate | 87-67-2 | C4H5O6*C5H14NO |
| 萘甲唑林 | naphazoline | 835-31-4 | C14H14N2 |
| 胆碱 | cholin hydroxide | 123-41-1 | C5H14NO*HO |
| 胆碱 | choline | 62-49-7 | C5H14NO |
| 硝酸毛果芸香碱 | pilocarpine nitrate | 148-72-1 | C11H16N2O2*HNO3 |
| 石杉碱甲 | huperzine A | 102518-79-6 | C15H18N2O |
| 石杉碱甲 | natural Huperzine A | 102518-79-6 | C15H18N2O |
| 盐酸萘甲唑啉 | naphazoline hydrochloride | 550-99-2 | C14H14N2*ClH |
| 盐酸四氢唑林 | tetryzoline hydrochloride | 522-48-5 | C13H16N2*ClH |
| 甲基硫酸新斯的明 | neostigmine methyl sulfate | 51-60-5 | CH3O4S*C12H19N2O2 |
| 甘磷酸胆碱 | L-glycero-3-phosphorylcholine | 28319-77-9 | C8H20NO6P |
| 溴吡斯的明 | pyridostigmine bromide | 101-26-8 | Br*C9H13N2O2 |
| 溴化新斯的明 | Neostigmine bromide | 114-80-7 | Br*C12H19N2O2 |
| 氯化胆碱 | choline chloride | 67-48-1 | C5H14NO*Cl |
| 氯化乙酰胆碱 | acetylcholine chloride | 60-31-1 | C7H16NO2*Cl |
| 氯化乙酰甲胆碱 | metacholine chloride | 62-51-1 | C8H18NO2*Cl |
| 氢溴酸加兰他敏 | 5-Methoxy-9-methyl-2,3,3a,3a1,8,9,10,11-octahydro-4-oxa-9-azacycloocta[def]fluoren-2-ol hydrobromide | 69353-21-5 | C17H22BrNO3 |
| 氢溴酸加兰他敏 | Galantamine hydrobromide | 1953-04-4 | BrH*C17H21NO3 |
| 毛果芸香碱 | pilocarpine | 92-13-7 | C11H16N2O2 |
| 毒扁豆碱 | Physostigmin | 57-47-6 | C15H21N3O2 |
| 山莨菪碱氢溴酸 | Anisodamine hydrobromide | 17659-49-3 | C17H24BrNO4 |
| 山莨菪碱 | (-)-Anisodamine | 55869-99-3 | C17H23NO4 |
| 外消旋山莨菪碱 | 7β-Hydroxyhyoscyamine | 17659-49-3 | C17H23NO4 |
| 地美溴铵 | Demecarium Bromide | 56-94-0 | C32H52Br2N4O4 |
| 四氢唑林 | tetrahydrozoline | 84-22-0 | C13H16N2 |
| 后马托品 | Homatropine | 87-00-3 | C16H21NO3 |
| 右苄替米特 | Dexetimide | 21888-98-2 | C23H26N2O2 |
| 卡巴胆碱 | carbachol | 51-83-2 | C6H15N2O2*Cl |
| 加兰他敏 | (-)-narwedine | 510-77-0 | C17H19NO3 |
| 伊色林 水杨酸盐 | eserine salicylate | 57-64-7 | C7H6O3*C15H21N3O2 |
| 二氢加兰他敏 | (-)-lycoramine | 21133-52-8 | C17H23NO3 |
| 乙酰胆碱 | acetylcholine | 51-84-3 | C7H16NO2 |
| 东莨菪碱氢溴酸盐 | Scopolamine hydrobromide | 114-49-8 | BrH*C17H21NO4 |
| 东莨菪碱 | Scopolamine | 51-34-3 | C17H21NO4 |
| 2-((氨基羰基)氧基)-N,N,N-三甲基乙铵 | Carbamoylcholine | 462-58-8 | C6H15N2O2+ |
| —— | 3-Bicyclo[3.2.1]octanyl 3-hydroxy-2-phenyl-propanoate | 55869-99-3 | C17H23NO4 |
| —— | [(1S,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate;sulfuric acid | 55-48-1 | C34H48N2O10S |
| —— | N6-p-Methoxyphenyladenosin | 510-77-0 | C17H19NO3 |
| —— | (-)-pilocarpine; nitrate | 148-72-1 | C11H16N2O2*HNO3 |
| —— | Homatropin-methobromid | 80-49-9 | Br*C17H24NO3 |
| —— | [(1R,2R,4S,5S)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2R)-3-hydroxy-2-phenylpropanoate;hydrobromide | 114-49-8 | C17H21NO4.BrH |
| —— | Transderm scop (TN) | 51-34-3 | C17H21NO4 |
| —— | Scopolamine | 51-34-3 | C17H21NO4 |
| —— | (-)-Homatropine | 51017-31-3 | C16H21NO3 |
| —— | (-)-huperzine A | 102518-79-6 | C15H18N2O |
| —— | Atroscine | 51-34-3 | C17H21NO4 |
| —— | Lopac-S-1875 | 51-34-3 | C17H21NO4 |
| —— | Atropine sulfate monohydrate | 55-48-1 | C34H50N2O11S |
| —— | Sdccgsbi-0051046.P002 | 51-34-3 | C17H21NO4 |
| —— | Isoptpo Hyoscine | 51-34-3 | C17H21NO4 |