激动剂抑制剂
激动剂和抑制剂
在生物化学和药物化学领域中，激动剂和抑制剂是调节受体活性的重要分子类型。
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激动剂：激动剂是指能够与特定受体结合并激活该受体，从而引起细胞内信号传递的化合物。它们通过与受体的特定位点相互作用，模拟天然配体的功能，导致生物效应的发生或增强。根据其对受体的作用机制不同，激动剂可以分为完全激动剂和部分激动剂。
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完全激动剂：能够完全激活受体，达到最大生物活性。
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部分激动剂：仅能部分地激活受体，即使在高浓度下也不表现出最大效应。
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抑制剂：抑制剂则是相反的一类分子，它们通过与受体或其相关蛋白质结合来阻止信号传导过程。根据作用机制的不同，可以分为竞争性抑制剂和非竞争性抑制剂。
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竞争性抑制剂：这些物质通过占据活性位点而减少激动剂的结合能力，通常可以通过增加激动剂浓度来克服这种抑制效应。
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非竞争性抑制剂：这类抑制剂不依赖于受体结合部位，而是通过其他方式干扰信号传递，如改变受体构象或直接与G蛋白相互作用。
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在药物研发过程中，激动剂和抑制剂的研究至关重要。它们不仅用于治疗疾病，还可以帮助理解生物系统的工作原理。例如，在神经科学领域，激动剂可以被用作治疗抑郁、焦虑等精神疾病的药物；而在癌症研究中，则可能使用抑制剂来阻断促进肿瘤生长的信号通路。
| 中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
|---|---|---|---|---|
| 4-((1,4-二氧代-1,4-二氢萘-2-基)氨基)苯磺酰胺 | 4-((1,4-dioxo-1,4-dihydronaphthalen-2-yl)amino)benzenesulfonamide | 19992-50-8 | C16H12N2O4S |
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| 4,6-二氯吲哚-2-甲酸 | 4,6-dichloro-1H-indole-2-carboxylic acid | 101861-63-6 | C9H5Cl2NO2 |
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| 4,5,6,7-四溴苯甲腈 | 4,5,6,7-tetrabromobenzotriazole | 17374-26-4 | C6HBr4N3 |
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| 4,4’-二乙酰胺基二苯基甲烷 | N,N'-diacetyl-4,4'-methylenedianiline | 2719-05-3 | C17H18N2O2 |
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| 4'-[4-[[[(1R)-1-(2-氯苯基)乙氧基]羰基]氨基]-3-甲基-5-异恶唑基]-联苯-4-乙酸 | AM966 | 1228690-19-4 | C27H23ClN2O5 |
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| 4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐 | AM095 | 1345614-59-6 | C27H23N2O5*Na |
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| 4'-C-迭氮基胞嘧啶核苷 2',3',5'-三异丁酸酯 | balapiravir | 690270-29-2 | C21H30N6O8 |
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| 4'-(环丙基甲基)-N2-4-吡啶基[4,5'-联嘧啶]-2,2'-二胺 | PIK-III | 1383716-40-2 | C17H17N7 |
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| 3，5-双[[（4-甲基苯基）亚甲基]-4-哌啶酮盐酸盐 | NSC 632839 hydrochloride | 157654-67-6 | C21H22ClNO |
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| 3-苯基-4-氨基丁酸盐酸盐 | 4-amino-3-phenylbutanoic acid hydrochloride | 3060-41-1 | C10H13NO2*ClH |
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| 3-苯基-2-异恶唑啉-5-乙酸 | VGX1027 | 6501-72-0 | C11H11NO3 |
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| 3-苯基-2-[4-[[4-[5-(2-吡啶)-1H-1,2,4-三唑-3-基]-1-哌啶]甲基]苯基]-1,6-萘啶-5(6H)-酮 | 3-phenyl-2-(4-{[4-(5-pyridin-2-yl-1H-1,2,4-triazol-3-yl)piperidin-1-yl]methyl}phenyl)-1,6-naphthyridin-5(6H)-one | 893422-47-4 | C33H29N7O |
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| 3-苄基-2-[(1E)-2-(3-吡啶基)乙烯基]-4(3H)-喹唑啉酮 | 3-(phenylmethyl)-2-[(1E)-2-(3-pyridinyl)ethenyl]-4(3H)-quinazolinone | 1290541-46-6 | C22H17N3O |
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| 3-羧基-4-辛基-2-亚甲基丁内酯 | trans-4-carboxy-5-octyl-3-methylene-butyrolactone | 218137-86-1 | C14H22O4 |
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| 3-氰基-N-(3-氰基-4-甲基-1H-吲哚-7-基)苯磺酰胺 | E7820 | 289483-69-8 | C17H12N4O2S |
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| 3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮 | 6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile | 491871-58-0 | C18H11BrN2O2 |
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| 3-氯-N-[反式-4-(甲基氨基)环己基]-N-[[3-(4-吡啶基)苯基]甲基]-苯并[b]噻吩-2-甲酰胺 | SAG | 912545-86-9 | C28H28ClN3OS |
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| 3-氯-2-甲基-N-(4-(2-(4-甲基哌嗪-1-基)-2-氧代乙基)噻唑-2-基)苯磺酰胺 | 3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide | 376640-41-4 | C17H21ClN4O3S2 |
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| 3-氯-1-(3,4-二氯苯基)-4-(4-吗啉基)-1H-吡咯-2,5-二酮 | (3-chloro-1-(3,4-dichlorophenyl)-4-(4-morpholinyl)-1H-pyrrole-2,5-dione) | 415713-60-9 | C14H11Cl3N2O3 |
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| 3-氨基-6-氯-5-[(3S)-4-[1-[(4-氯苯基)甲基]-4-哌啶基]-3-乙基-1-哌嗪基]-2-哌嗪甲酰胺 | (S)-3-Amino-6-chloro-5-(4-(1-(4-chlorobenzyl)piperidin-4-yl)-3-ethylpiperazin-1-yl)pyrazine-2-carboxamide | 906805-42-3 | C23H31Cl2N7O |
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| 3-四聚丙烯基二氢-2,5-呋喃二酮 | 3-(4-methyl-2-{[(3Z)-2-oxo-1H-indol-3-ylidene]methyl}-1H-pyrrol-3-yl)propanoic acid | 215543-92-3 | C17H16N2O3 |
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| 3-乙基-2-苯并咪唑酮 | N-ethylbenzimidazolinone | 10045-45-1 | C9H10N2O |
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| 3-乙基-1-丙基-8-(1-(3-(三氟甲基)苄基)-1H-吡唑-4-基)-1H-嘌呤-2,6(3H,8H)-二酮 | 3-ethyl-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]-7H-purine-2,6-dione | 752222-83-6 | C21H21F3N6O2 |
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| 3-{3-[4-(1-甲基-1H-吲哚-3-基)-2,5-二羰基-2,5-二氢-1H-吡咯-3-基]-1H-吲哚-1-基}丙基氨基甲酰亚胺基硫酸酯 | Ro 31-8220 | 125314-64-9 | C25H23N5O2S |
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| 3-[[[3-[4-[(甲基磺酰基)氨基]苯基]-4-氧代-4H-苯并吡喃-7-基]氧基]甲基]苯甲酸 | CVT-10216 | 1005334-57-5 | C24H19NO7S |
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| 3-[[[2-甲氧基-4-(苯基氨基)苯基]氨基]磺酰基]-2-噻吩羧酸甲酯 | GSK0660 | 1014691-61-2 | C19H18N2O5S2 |
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| 3-[[6-(乙基磺酰基)-3-吡啶基]氧基]-5-[(1S)-2-羟基-1-甲基乙氧基]-N-(1-甲基-1H-吡唑-3-基)苯甲酰胺甲烷磺酸盐 | 3-(6-ethanesulfonylpyridin-3-yloxy)-5-((S)-2-hydroxy-1-methylethoxy)-N-(1-methyl-1H-pyrazol-3-yl)benzamide methanesulfonic acid salt | 1137916-97-2 | CH4O3S*C21H24N4O6S |
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| 3-[[5-(4-甲基苯基)噻吩并[2,3-d]嘧啶-4-基]硫代]丙酸 | 3-{[5-(4-methylphenyl)thieno[2,3-d]pyrimidin-4-yl]thio}propanoic acid | 329907-28-0 | C16H14N2O2S2 |
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| 3-[[4-[(5-羟基-2-甲基苯基)氨基]-2-嘧啶基]氨基]苯甲酰胺 | Lck inhibitor 2 | 944795-06-6 | C18H17N5O2 |
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| 3-[[3-[(二甲氨基)羰基]-2-羟基苯基]氨基]-4-[[(R)-1-(4-异丙基呋喃-2-基)丙基]氨基]环丁-3-烯-1,2-二酮 | SCH563705 | 473728-58-4 | C23H27N3O5 |
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| 3-[[((2-甲基苯基)甲基]硫代]-6-(2-吡啶基)-哒嗪 | (3-[(2-methylbenzyl)sulfenyl]-6-(pyridine-2-yl)pyridazine) | 894002-50-7 | C17H15N3S |
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| 3-[3-[[[2-氯-3-(三氟甲基)苯基]甲基](2,2-联苯基乙基)氨基]丙氧基]苯乙酸盐酸盐 | 3-[3-[[[2-chloro-3-(trifluoromethyl)phenyl]methyl](2,2-diphenylethyl)amino]propoxy]benzeneacetic acid | 405911-09-3 | C33H31ClF3NO3 |
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| 3-[3-[[(甲基氨基)羰基]氧基]丙基]-1-丙基-2(1H)-喹喔啉酮 | 1-propyl 3-(3-methylcarbamoyloxy propyl) 1,2-dihydro 2-oxo quinoxaline | 135779-82-7 | C16H21N3O3 |
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| 3-[3-[4-(1-氨基环丁基)苯基]-5-苯基-3H-咪唑并[4,5-b]吡啶-2-基]-2-吡啶胺 | ARQ-092 | 1313881-70-7 | C27H24N6 |
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| 3-[3-[2-(1-哌啶基)乙氧基]苯基]-5-(1H-1,2,4-三唑-5-基)-1H-吲唑 | 1-(5-(1H-1,2,4-triazol-3-yl)(1H-indazol-3-yl))-3-(2-piperidylethoxy)benzene | 395104-30-0 | C22H24N6O |
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| 3-[3-[(环己基羰基)[[4'-(二甲基氨基)[1,1'-联苯]-4-基]甲基]氨基]苯基]-2-丙烯酸甲酯 | fexaramine | 574013-66-4 | C32H36N2O3 |
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| 3-[2-(三氟甲基)苄氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺 | GW843682X | 660868-91-7 | C22H18F3N3O4S |
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| 3-[1-(4-氯苄基)-3-叔丁基硫代-5-异丙基吲哚-2-基]-2,2-二甲基丙酸 | 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid | 118414-82-7 | C27H34ClNO2S |
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| 3-[(4-溴-2,6-二氟苄基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]异噻唑-4-甲酰胺 | 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]amino]carbonyl]amino]-4-isothiazolecarboxamide | 252003-65-9 | C20H24BrF2N5O3S |
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| 3-[(2-甲基-2H-吲唑-5-基)硫基]-6-(1-甲基-1H-吡唑-4-基)-1,2,4-三唑并[4,3-b]哒嗪 | 6-(1-methyl-1H-pyrazol-4-yl)-3-(2-methyl-2H-indazol-5-ylthio)-[1,2,4]triazolo[4,3-b]pyridazine | 1357072-61-7 | C17H14N8S |
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| 3-[(2-甲基-2-丙烯-1-基)硫基]-5H-1,2,4-三嗪并[5,6-b]吲哚 | 3-[(2-methylprop-2-en-1-yl)sulfanyl]-5H-[1,2,4]triazino[5,6-b]indole | 328023-11-6 | C13H12N4S |
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| 3-[(2-氨基-6-甲基-3-吡啶基)甲基]-5-(2-羟基乙基)-4-甲基噻唑鎓氯化物盐酸盐 | 3-(2-amino-6-methyl-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride | 13860-66-7 | C13H18N3OS*ClH*Cl |
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| 3-[(1S,2S)-2-羟基环己基]-6-[(6-甲基-3-吡啶基)甲基]苯并[h]喹唑啉-4(3H)-酮 | MK-7622 | 1227923-29-6 | C25H25N3O2 |
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| 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 | (E)-4,6-dichloro-3-(2-phenyl-2-carboxyethenyl)indole-2-carboxylic acid | 161230-88-2 | C18H11Cl2NO4 |
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| 3-(甲氨基)甲苯 | N-methyl-m-toluidine | 696-44-6 | C8H11N |
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| 3-(乙酰氨基)丙烷磺酸钙 | 77337-73-6 | C5H11CaNO4S |
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| 3-(6-(二甲基氨基)-4-甲基吡啶-3-基)-2,5-二甲基-N,N-二丙基吡唑并[1,5-a]嘧啶-7-胺 | 3-[6-(dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[2,3-a]pyrimidine-7-amine | 195055-03-9 | C22H32N6 |
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| 3-(5-羟基甲基-2-呋喃基)-1-苯基吲哚 | 1-benzyl-3-(5-hydroxymethyl-2-furyl)indazole | 170632-47-0 | C19H16N2O2 |
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| 3-(5-氨基-2-甲基-4-氧喹唑啉-3(4H)-基)哌啶-2,6-二酮 | 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione | 1015474-32-4 | C14H14N4O3 |
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| 3-(5-氟-吲哚-3-基)-吡咯烷-2,5-二酮 | PF-06840003 | 198474-05-4 | C12H9FN2O2 |
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