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。
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。
完全激动剂:能够完全激活受体,达到最大生物活性。
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。
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。
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。
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。
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 |
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1-乙基-1,2-二氢-4-羟基-2-氧代-3-喹啉羧酸 2-(1-氧代十三烷基)酰肼 | 1-ethyl-4-hydroxy-2-oxo-N'-tridecanoyl-1,2-dihydroquinoline-3-carbohydrazide | 331963-29-2 | C25H37N3O4 |
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1-丁基-3-氯-4-(4-苯基哌啶-1-基)吡啶-2(1H)-酮 | 1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2(1H)-one | 1127498-03-6 | C20H25ClN2O |
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1-[β-(3-(4-甲氧基苯基)丙氧基)-4-甲氧苯]-1H-咪唑盐酸盐 | SKF 96365 | 130495-35-1 | C22H26N2O3*ClH |
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1-[[3,4-二氟-2-[(2-氟-4-碘苯基)氨基]苯基]羰基]-3-(哌啶-2-基)氮杂环丁-3-醇 | cobimetinib | 934662-91-6 | C21H21F3IN3O2 |
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1-[[1,5-二(4-氯苯基)-2-甲基-1H-吡咯-3-基]甲基]-4-甲基哌嗪 | 1-((1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine | 146204-42-4 | C23H25Cl2N3 |
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1-[[(2S,3S,4S)-3-乙基-4-氟-5-氧代-2-吡咯烷基]甲氧基]-7-甲氧基-6-异喹啉羧酰胺 | PF06650833 | 1817626-54-2 | C18H20FN3O4 |
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1-[6-(3,5-二氯-4-羟基苯基)-4-[[反式-4-[(二甲基氨基)甲基]环己基]氨基]-1,5-萘啶-3-基]-乙酮 | OTSSP167 | 1431697-89-0 | C25H28Cl2N4O2 |
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1-[4-[2-羟基-3-(5-喹啉基氧基)丙基]-1-哌嗪基]-2,2-二苯基乙酮 | 5-[3-(4-(2,2-diphenylacetyl)piperazine-1-yl)-2-hydroxypropoxy]quinoline | 129716-58-1 | C30H31N3O3 |
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1-[4-(2-萘基)-2-嘧啶基]-4-哌啶甲胺 | WAY-262611 | 1123231-07-1 | C20H22N4 |
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1-[3-[2-[4-(2-甲基-5-喹啉基)-1-哌嗪基]乙基]苯基]-2-咪唑烷酮 | 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone | 844903-58-8 | C25H29N5O |
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1-[3-(4-溴-1-甲基-1H-吡唑-5-基)-4-甲氧基苯基]-3-(2,4-二氟苯基)脲 | Nelotanserin | 839713-36-9 | C18H15BrF2N4O2 |
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1-[3,5-二(1,1-二甲基乙基)-4-羟基苯基]-2-[2-[(3-羟基丙基)氨基]-5,6-二甲基-1H-苯并咪唑-1-基]-乙酮 | AJW-200 | 758679-97-9 | C28H39N3O3 |
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1-[2-氟-4-(1H-吡唑-1-基)苯基]-5-甲氧基-3-(1-苯基-1H-吡唑-5-基)哒嗪-4(1H)-酮 | 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one | 1238697-26-1 | C23H17FN6O2 |
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1-[2-(二苯基甲氧基)乙基]-4-(3-苯基-2-丙苯基)-哌嗪 | 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl-2-propenyl)piperazine | 67469-57-2 | C28H32N2O |
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1-[2-(3,4-二甲氧基苯基)乙基]-4-(3-苯基丙基)哌嗪盐酸盐 | 1-(3,4-Dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride | 165377-44-6 | C23H34Cl2N2O2 |
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1-[1-[(5-甲氧基-1H-吲哚-2-基)羰基]哌啶-4-基]-2-甲基丙-2-醇 | ASP9521 | 1126084-37-4 | C19H26N2O3 |
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1-[1-[(2-氨基吡啶-4-基)甲基]-1H-吲哚-4-基]-3-(5-溴-2-甲氧基苯基)脲 | 1-[1-(2-amino-pyridin-4-ylmethyl)-1H-indol-4-yl]-3-(5-bromo-2-methoxy-phenyl)-urea | 900573-88-8 | C22H20BrN5O2 |
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1-[1-(1-甲基环辛基)-4-哌啶基]-2-[(3R)-3-哌啶基]-1H-苯并咪唑 | 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole | 1028969-49-4 | C26H40N4 |
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1-[(4-氯苯基)甲基]-5-(三氟甲基)苯并咪唑-2-胺 | 2-amino-1-(4-chlorobenzyl)-5-trifluoromethylbenzimidazole | 150493-34-8 | C15H11ClF3N3 |
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1-[(4,6-二甲基-5-嘧啶基)羰基]-4-[(3S)-4-[(1R)-2-甲氧基-1-[4-(三氟甲基)苯基]乙基]-3-甲基-1-哌嗪基]-4-甲基哌啶马来酸盐 | Vicriviroc maleate | 599179-03-0 | C32H42F3N5O6 |
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1-[(3S)-3-[4-氨基-3-[2-(3,5-二甲氧基苯基)乙炔基]-1H-吡唑并[3,4-d]嘧啶-1-基]-1-吡咯烷基]-2-丙烯-1-酮 | futibatinib | 1448169-71-8 | C22H22N6O3 |
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1-(二苯基甲基)-4-(1-氧代-3,3-二苯基丙基)哌嗪 | NP118809 | 41332-24-5 | C32H32N2O |
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1-(4-苯甲酰基哌嗪-1-基)-2-[4-甲氧基-7-(3-甲基-1H-1,2,4-三氮唑-1-基)-1H-吡咯并[2,3-c]吡啶-3-基)乙烷-1,2-二酮 | 1-(4-benzoylpiperazin-1-yl)-2-(4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)-ethane-1,2-dione | 701213-36-7 | C24H23N7O4 |
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1-(4-羟基环己基)-2-[[5-(2-三氟甲氧基苯基)-1H-吲唑-3-基]氨基]-1H-苯并咪唑-5-羧酸(3-甲基丁基)酰胺 | 2-(5-(2-(trifluoromethoxy)phenyl)-1H-indazol-3-ylamino)-1-(4-hydroxycyclohexyl)-N-isopentyl-1H-benzo[d]imidazole-5-carboxamide | 1012104-68-5 | C33H35F3N6O3 |
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1-(4-甲氧基苯基)-2-甲基-3-硝基-1H-吲哚-6-醇 | ID-8 | 147591-46-6 | C16H14N2O4 |
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1-(4-氰基-2-吡啶基)-5-氧代-L-脯氨酰-2-(2-氯苯基)-N-(3,3-二氟环丁基)-N2-(5-氟-3-吡啶基)甘氨酰胺 | (2S)-N-(1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide | 1448346-63-1 | C28H22ClF3N6O3 |
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1-(4-氟苯基)-N-[3-氟-4-(1H-吡咯并[2,3-B]吡啶-4-基氧基)苯基]-1,2-二氢-2-氧代-3-吡啶甲酰胺 | BMS-2 | 888719-03-7 | C25H16F2N4O3 |
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1-(4-乙氧羰基苯基)-2-(4-氟苄基硫基)-5-(2-乙氧基-5-嘧啶基甲基)-4-嘧啶酮 | GW1100 | 306974-70-9 | C27H25FN4O4S |
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1-(4-(苄基氨基)-7,8-二氢-5H-吡喃并[4,3-D]嘧啶-2-基)-2-甲基-1H-吲哚-4-甲酰胺 | CB-5083 | 1542705-92-9 | C24H23N5O2 |
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1-(4-(2H-四唑-5-基)丁基)-4-(5H-二苯并[A,D][7]环庚烯-5-亚基)哌啶 | 1-(4-(2H-tetrazol-5-yl)butyl)-4-(5H-dibenzo[a,d][7]annulen-5-ylidene)piperidine | 162640-98-4 | C25H27N5 |
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1-(4,4-二苯基-3-丁烯)-3-哌啶羧酸盐酸盐 | SKF 89976A | 85375-15-1 | C22H25NO2*ClH |
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1-(3-甲氧基苄基)-3-[4-(吡啶-4-基)噻唑-2-基]脲 | 1-(3-methoxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea | 1342276-76-9 | C17H16N4O2S |
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1-(3-氯-4-氟苯基)-4-[(5-硝基-2-呋喃基)亚甲基]-3,5-吡唑烷二酮 | 1-(3-Chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione | 423148-78-1 | C14H7ClFN3O5 |
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1-(3,6-二溴-9h-咔唑-9-基)-3-(二甲基氨基)-2-丙醇 | Wiskostatin | 253449-04-6 | C17H18Br2N2O |
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1-(3,6-二溴-9H-咔唑-9-基)-3-(苯基氨基)丙-2-醇 | 1-(3,6-dibromo-9H-carbazol-9-yl)-3-(phenylamino)propan-2-ol | 301353-96-8 | C21H18Br2N2O |
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1-(3,4-二氯苯基)-3-(4-甲氧基苯基)-4-(4-吗啉基)-1H-吡咯-2,5-二酮 | 1-(3,4-dichloro-phenyl)-3-(4-methoxy-phenyl)-4-morpholin-4-yl-pyrrole-2,5-dione | 1417162-36-7 | C21H18Cl2N2O4 |
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1-(2-羟基-5-(三氟甲基)苯基)-5-(三氟甲基)-1H-苯并[d]咪唑-2(3h)-酮 | NS 1619 | 153587-01-0 | C15H8F6N2O2 |
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1-(2-羟乙基)-2-硫代咪唑烷酮 | N-(2'-hydroxyethyl)imidazoline-2-thione | 932-49-0 | C5H10N2OS |
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1-(2-甲基-1,3-苯并恶唑-6-基)-3-(1,5-萘啶-4-基)脲 | SB 334867A | 249889-64-3 | C17H13N5O2*ClH |
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1-(2-氟-5-硝基苯基)-N-甲基-N-(1-甲基丙基)-3-异喹啉甲酰胺 | N-butan-2-yl-1-(2-fluoro-5-nitrophenyl)-N-methylisoquinoline-3-carboxamide | 107257-28-3 | C21H20FN3O3 |
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1-(2-二苯基甲氧基乙基)-4-(3-苯基丙基)哌嗪双盐酸盐 | GBR 12935 dihydrochloride | 67469-81-2 | C28H36Cl2N2O |
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1-(2,4-二氯苯基)-N-1-哌啶基-4-[[(1-吡咯烷基磺酰基)氨基]甲基]-5-[5-[2-[4-(三氟甲基)苯基]乙炔基]-2-噻吩基]-1H-吡唑-3-甲酰胺 | 1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-1H-pyrazole-3-carboxamide | 1429239-98-4 | C33H31Cl2F3N6O3S2 |
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1-(2,4-二氯苯基)-N-(2,4-二氟苯基)-1,5-二氢-N-异丙基-5-氧代-4H-1,2,4-三氮唑-4-甲酰胺 | Ipfencarbazone | 212201-70-2 | C18H14Cl2F2N4O2 |
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1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺 | N-(morpholin-4-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide | 202463-68-1 | C21H19Cl2IN4O2 |
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1-(2,3-二氢-1,4-苯并二烷-5-基)哌嗪盐酸盐 | eltoprazine | 98224-03-4 | C12H16N2O2 |
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1-(2,3-二氢-1,4-苯并二恶烷-5-基)-4-[[5-(4-氟苯基)-3-吡啶基]甲基]哌嗪 | Adoprazine | 222551-17-9 | C24H24FN3O2 |
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1-(1-(1-(乙基磺酰基)哌啶-4-基)乙基)-N-((4-甲氧基-6-甲基-2-氧代-1,2-二氢吡啶-3-基)甲基)-2-甲基-1H-吲哚-3-甲酰胺 | 1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide | 1450655-76-1 | C27H36N4O5S |
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1,5-酐-2,3-双脱氧-3-[[(1R,3S)-3-[[7,8-二氢-3-(三氟甲基)-1,6-萘啶-6(5H)-基]羰基]-3-(1-甲基乙基)环己基]氨基]-4-O-甲基-D-赤式-戊糖醇 | MK0812 | 624733-88-6 | C24H34F3N3O3 |
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1,5-二氢-6-[(3S,4S)-4-甲基-1-苄基-3-吡咯烷基]-1-(四氢-2H-吡喃-4-基)-4H-吡唑并[3,4-d]嘧啶-4-酮 | 6-((3S,4S)-1-benzyl-4-methylpyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one | 1082743-70-1 | C22H27N5O2 |
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1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯巯基)丁二烯 | 1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene | 109511-58-2 | C18H16N6S2 |
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