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拟胆碱药

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 结构式图片
—— [(3S,5S,6S)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2S)-3-hydroxy-2-phenylpropanoate 55869-99-3 C17H23NO4
[(3S,5S,6S)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2S)-3-hydroxy-2-phenylpropanoate
—— Etybenzatropine 524-83-4 C22H27NO
Etybenzatropine
—— (1S,9R,13E)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one 102518-79-6 C15H18N2O
(1S,9R,13E)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one
—— Atroscine Hydrobromide 672-21-9 C17H21NO4.BrH
Atroscine Hydrobromide
—— [(5R)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octan-3-yl] 2-hydroxy-2-phenylacetate;bromide 80-49-9 C17H24BrNO3
[(5R)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octan-3-yl] 2-hydroxy-2-phenylacetate;bromide
—— Atropine sulfate 5908-99-6 C34H48N2O10S
Atropine sulfate
—— Hyoscyamine sulfate monohydrate 5908-99-6 C34H50N2O11S
Hyoscyamine sulfate monohydrate
—— (1R,9S,13Z)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one 102518-79-6 C15H18N2O
(1R,9S,13Z)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one
—— Homatropine Methylbromide; (1R,3r,5S)-3-[[(2RS)-2-Hydroxy-2-phenylacetyl]oxy]-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide 80-49-9 C17H24BrNO3
Homatropine Methylbromide; (1R,3r,5S)-3-[[(2RS)-2-Hydroxy-2-phenylacetyl]oxy]-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide
—— (2-Chlorophenyl)methyl-[2-[[2-[2-[(2-chlorophenyl)methyl-diethylazaniumyl]ethylamino]-2-oxoacetyl]amino]ethyl]-diethylazanium;chloride 115-79-7 C28H42Cl3N4O2+
(2-Chlorophenyl)methyl-[2-[[2-[2-[(2-chlorophenyl)methyl-diethylazaniumyl]ethylamino]-2-oxoacetyl]amino]ethyl]-diethylazanium;chloride
—— Homatropine methylbromide 80-49-9 C17H24BrNO3
Homatropine methylbromide
—— (9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl) (2S)-3-hydroxy-2-phenylpropanoate;hydrobromide 114-49-8 C17H22BrNO4
(9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl) (2S)-3-hydroxy-2-phenylpropanoate;hydrobromide
—— [(1R,2S,4S,5S)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate 51-34-3 C17H21NO4
[(1R,2S,4S,5S)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate
—— (-)-huperzine A 102518-79-6 C15H18N2O
(-)-huperzine A
—— lycoramine 18797-70-1 C17H23NO3
lycoramine
—— [(4R)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] 3-hydroxy-2-phenylpropanoate 51-34-3 C17H21NO4
[(4R)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] 3-hydroxy-2-phenylpropanoate
—— [(1S,3S,5R,6S)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2S)-3-hydroxy-2-phenylpropanoate 55869-99-3 C17H23NO4
[(1S,3S,5R,6S)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2S)-3-hydroxy-2-phenylpropanoate
—— [(2S,4R)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] 2,3-dihydroxy-2-phenylpropanoate;hydrobromide 76822-34-9 C17H22BrNO5
[(2S,4R)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] 2,3-dihydroxy-2-phenylpropanoate;hydrobromide
—— [(1R)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2S)-3-hydroxy-2-phenylpropanoate 55869-99-3 C17H23NO4
[(1R)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2S)-3-hydroxy-2-phenylpropanoate
—— (-)-Scopolamine hydrobromide 114-49-8 C17H22BrNO4
(-)-Scopolamine hydrobromide
—— 6-Hydroxyhyoscyamine 55869-99-3 C17H23NO4
6-Hydroxyhyoscyamine
—— [(1S,5S)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate 55869-99-3 C17H23NO4
[(1S,5S)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate
—— [(2R,4S)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2R)-3-hydroxy-2-phenylpropanoate 51-34-3 C17H21NO4
[(2R,4S)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2R)-3-hydroxy-2-phenylpropanoate
—— cuscohygrine 454-14-8 C13H24N2O
cuscohygrine
—— (12aξ)-6-methoxy-10-methyl-1,12-cyclo-12,12a-seco-galantham-1-en-3β-ol; hydrobromide 69353-21-5 BrH*C17H21NO3
(12aξ)-6-methoxy-10-methyl-1,12-cyclo-12,12a-seco-galantham-1-en-3β-ol; hydrobromide
—— 1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0<sup>2,7</sup>]trideca-2(7),3,10-trien-5-one 92138-20-0 C15H18N2O
1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0<sup>2,7</sup>]trideca-2(7),3,10-trien-5-one
—— (-)-huperzine A 120786-18-7 C15H18N2O
(-)-huperzine A
—— 3-hydroxy-2-phenyl-propionic acid 9-methyl-3-oxa-9-aza-tricyclo[3.3.1.0<sup>2,4</sup>]non-7-yl ester 51-34-3 C17H21NO4
3-hydroxy-2-phenyl-propionic acid 9-methyl-3-oxa-9-aza-tricyclo[3.3.1.0<sup>2,4</sup>]non-7-yl ester
—— 3-hydroxy-2-phenyl-propionic acid 9-methyl-(1<i>r</i><i>N</i>,2<i>t</i><i>H</i>,4<i>t</i><i>H</i>,5<i>c</i><i>N</i>)-3-oxa-9-aza-tricyclo[3.3.1.0<sup>2,4</sup>]non-7<i>t</i>-yl ester 51-34-3 C17H21NO4
3-hydroxy-2-phenyl-propionic acid 9-methyl-(1<i>r</i><i>N</i>,2<i>t</i><i>H</i>,4<i>t</i><i>H</i>,5<i>c</i><i>N</i>)-3-oxa-9-aza-tricyclo[3.3.1.0<sup>2,4</sup>]non-7<i>t</i>-yl ester
—— scopolamine 51-34-3 C17H21NO4
scopolamine
—— (-)-SCOPOLAMINE 138-12-5 C17H21NO4
(-)-SCOPOLAMINE
—— (+/-)-Pseudohomatropin 87-00-3 C16H21NO3
(+/-)-Pseudohomatropin
—— Demecarium bromide 56-94-0 2Br*C32H52N4O4
Demecarium bromide
—— Homatropine 87-00-3 C16H21NO3
Homatropine
—— 6β-Hydroxyhyoscyamine 17659-49-3 C17H23NO4
6β-Hydroxyhyoscyamine
—— L-tropic acid-((1Ξ)-6<i>exo</i>-hydroxy-tropane-3<i>endo</i>-yl ester) 17659-49-3 C17H23NO4
L-tropic acid-((1Ξ)-6<i>exo</i>-hydroxy-tropane-3<i>endo</i>-yl ester)
—— homatropine methyl bromide 80-49-9 CH3Br*C16H21NO3
homatropine methyl bromide
—— homatropine methylbromide 80-49-9 Br*C17H24NO3
homatropine methylbromide
—— homatropine hydrobromide 51-56-9 BrH*C16H21NO3
homatropine hydrobromide
—— DL-Homatropine hydrobromide 51-56-9 BrH*C16H21NO3
DL-Homatropine hydrobromide
—— Ethybenztropine 524-83-4 C22H27NO
Ethybenztropine
—— Scopolamine hydrobromide trihydrate 114-49-8 C17H28BrNO7
Scopolamine hydrobromide trihydrate
—— HYOSCYAMINE SULFATE 5908-99-6 C17H23NO3*H2O*H2O4S
HYOSCYAMINE SULFATE
—— Atropine 51-55-8 C17H23NO3
Atropine
—— atropine 51-55-8 C17H23NO3
atropine
—— choline Bitartrate 87-67-2 C4H5O6*C5H14NO
choline Bitartrate
—— huperzine A 120786-18-7 C15H18N2O
huperzine A
—— 6-Hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 3-hydroxy-2-phenylpropanoate 55869-99-3 C17H23NO4
6-Hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 3-hydroxy-2-phenylpropanoate
—— physostigmine 57-47-6 C15H21N3O2
physostigmine