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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1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯巯基)丁二烯 | U0126 | 218601-62-8 | C18H16N6S2 |
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1,4-二氢-2,6-二甲基-5-硝基-4-(2-[三氟甲基]苯基)吡啶-3-羧酸甲酯 | 1,4-dihydro-2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]pyridine-3-carboxylic acid methyl ester | 71145-03-4 | C16H15F3N2O4 |
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1,3-二氢-8-[5-(1-羟基-1-甲基乙基)-3-吡啶基]-1-[(2S)-2-甲氧基丙基]-3-甲基-2H-咪唑并[4,5-c]喹啉-2-酮 | 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one | 1386874-06-1 | C23H26N4O3 |
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1,3-二氢-1-[1-[[4-(6-苯基-1H-咪唑并[4,5-G]喹喔啉-7-基)苯基]甲基]-4-哌啶基]-2H-苯并咪唑-2-酮 | Akt inhibitor VIII | 612847-09-3 | C34H29N7O |
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1,3-二(4-氨基苯基)脲 | N,N'-bis(4-aminophenyl)urea | 4550-72-5 | C13H14N4O |
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1,2-二氢-2-[6-(4-吗啉基)-4-嘧啶基]-4-(1H-1,2,3-三唑-1-基)-3H-吡唑-3-一 | molidustat | 1154028-82-6 | C13H14N8O2 |
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1,2,3,6-四氢-1,3-二甲基-2,6-二氧代-N-(6-苯基-3-哒嗪基)-7H-嘌呤-7-乙酰胺 | 2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide | 1638250-96-0 | C19H17N7O3 |
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1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐 | 1-(naphthalen-1-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol Hydrobromide | 132836-42-1 | C20H20BrNO2 |
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1',3'-二氢-2H-螺[咪唑并[1,2-A]吡啶-3,2'-茚]-2-酮 | ZSET1446 | 887603-94-3 | C15H12N2O |
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-联苯]-4-基甲基)-6-苯基-3-(2-吡啶基)-1,2,4-三嗪-5-胺 | ML228 | 1357171-62-0 | C27H21N5 |
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-[3-甲基-4-[[[((R)-1-苯基乙基)氧基]羰基]氨基]异恶唑-5-基]联苯-4-基]环丙烷羧酸 | BMS-986020 | 1257213-50-5 | C29H26N2O5 |
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(alphaS)-alpha-[4-(1H-吡唑-1-基)苯基]-alpha-(三氟甲基)-5-[[1-(三氟甲基)环丙基]甲基]-1H-咪唑-2-乙醇 | MK-5046 | 1022152-70-0 | C20H18F6N4O |
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(alphaS)-7-氟-alpha-甲基-N-9H-嘌呤-6-基-2-(2-吡啶基)-3-喹啉甲胺 | (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine | 1608125-21-8 | C21H16FN7 |
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(alphaR,betaS)-alpha-(4-羟基苯基)-beta-甲基-4-苄基-1-哌啶丙醇 | 4-[(1R,2S)-3-(4-Benzyl-piperidin-1-yl)-1-hydroxy-2-methyl-propyl]-phenol | 169274-78-6 | C22H29NO2 |
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(Z)-辣椒素 | cis-capsaicin | 25775-90-0 | C18H27NO3 |
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(Z)-N-去甲基-4-羟基三苯氧胺 | (Z)-endoxyfen | 112093-28-4 | C25H27NO2 |
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(Z)-2-癸烯酸 | cis-2-decenoic acid | 15790-91-7 | C10H18O2 |
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(S)-[4-(3-氟-5-三氟甲基吡啶-2-基)哌嗪-1-基][5-(甲磺酰基)-2-(2,2,2-三氟-1-甲基乙氧基)苯基]甲酮 | Bitopertin | 845614-11-1 | C21H20F7N3O4S |
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(S)-N-[2-(2-氰基-4,4-二氟-1-吡咯烷基)-2-氧代乙基]喹啉-4-甲酰胺 | (S)-N-(2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)quinoline-4-carboxamide | 1448440-52-5 | C17H14F2N4O2 |
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(S)-N-(2-丙炔基)-2,3-二氢茚-1-胺 | N-Propargyl-1(S)-aminoindan | 185517-74-2 | C12H13N |
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(S)-ALPHA-氨基-2'-氯-5-(膦酰甲基)-[1,1'-联苯]-3-丙酸盐酸盐 | SDZ 220-581 hydrochloride | 179411-93-9 | C16H18Cl2NO5P |
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(S)-6,7-二氢-2-硝基-6-[[4-(三氟甲氧基)苯基]甲氧基]-5H-咪唑并[2,1-B][1,3]恶嗪 | PA-824 | 187235-37-6 | C14H12F3N3O5 |
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(S)-3-(氨基甲基)-7-(3-羟基丙氧基)苯并[c][1,2]噁硼烷-1(3h)-醇 | (S)-3-(aminomethyl)-7-(3-hydroxypropoxy)benzo[c][1,2]oxaborol-1(3H)-ol hydrochloride | 1234563-16-6 | C11H16BNO4*ClH |
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(S)-3-(4-((4-(三氟甲基)-[1,1-联苯]-3-基)甲氧基)苯基)-4-己酸 | AMG 837 | 865231-46-5 | C26H21F3O3 |
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(S)-2-[[4-[(2-氟苄基)氧基]苄基]氨基]丙酰胺 | ralfinamide | 133865-88-0 | C17H19FN2O2 |
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(S)-2-[[2-[5-(5-甲脒基-1H-苯并咪唑-2-基)-6,2'-二羟基-5'-氨基磺酰基联苯-3-基]乙酰基]氨基]琥珀酸 | (S)-2-{2-[5-(5-carbamimidoyl-1H-benzimidazol-2-yl)-6,2'-dihydroxy-5'-sulfamoylbiphenyl-3-yl]acetylamino}succinic acid | 871266-63-6 | C26H24N6O9S |
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(S)-2-(2,6-二氯苯酰胺)-3-(2,6-二甲氧基-[1,1-联苯]-4-基)丙酸 | [14C]-TR-14035 | 232271-19-1 | C24H21Cl2NO5 |
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(S)-2-((S)-2-(二甲基氨基)-3-甲基丁酰氨基)-N-((3R,4S,5S)-3-甲氧基-1-((s)-2-((1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(((S)-2-苯基-1-(噻唑-2-基)乙基)氨基)丙基)吡咯烷-1-基)-5-甲基-1-氧代庚烷-4-基)-N,3-二甲基丁酰胺 | dolastatin 10 | 110417-88-4 | C42H68N6O6S |
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(S)-1-[5-[2-氟苯基]-2-甲基噻唑-4-基]-1-[2-[[5-苯基-[1,3,4]恶二唑-2-基]甲基]吡咯烷-1-基]甲酮 | [5-(2-fluorophenyl)-2-methyl-1,3-thiazol-4-yl]-[(2S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]pyrrolidin-1-yl]methanone | 483313-22-0 | C24H21FN4O2S |
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(S)-1-(1-(4-氯-3-氟苯基)-2-羟乙基)-4-(2-((1-甲基-1H-吡唑-5-基)氨基)嘧啶-4-基)吡啶-2(1H)-酮 | GDC-0994 | 1453848-26-4 | C21H18ClFN6O2 |
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(S)-(+)-布洛芬 | (S)-ibuprofen | 51146-56-6 | C13H18O2 |
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(R)-萘普生 | (R)-2-(6-methoxy-2-naphthyl)propionic acid | 23979-41-1 | C14H14O3 |
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(R)-9-[4-[1-(二甲基氨基)丙-2-基]苯基]-8-羟基-6-甲基噻吩并[2,3-C]喹啉-4(5H)-酮盐酸盐 | OTS964 | 1338545-07-5 | C23H24N2O2S*ClH |
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(R)-5,6-二氢-5-(甲基氨基)-4H-咪唑并[4,5,1-ij]喹啉-2(1H)-酮马来酸盐 | Sumanirole maleate | 179386-44-8 | C4H4O4*C11H13N3O |
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(R)-4A-(乙氧基甲基)-1-(4-氟苯基)-6-((4-(三氟甲基)苯基)磺酰基)-4,4A,5,6,7,8-六氢-1H-吡唑并[3,4-G]异喹啉 | (R)-4-a-ethoxymethyl-1-(4-fluoro-phenyl)-6-(4-trifluoromethyl-benzenesulfonyl)-4,4a,5,6,7,8-hexahydro-1H,1,2,6-triaza-cyclopenta[b]naphthalene | 1018679-79-2 | C26H25F4N3O3S |
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(R)-4-(2-(2-(2-甲基吡咯烷-1-基)乙基)苯并呋喃-5-基)苯甲腈 | 4-{2-[2-(2R-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl}benzonitrile | 460746-46-7 | C22H22N2O |
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(R)-4-((二乙基氨基)甲基)-n-(2-甲氧基苯乙基)-n-(吡咯烷-3-基)苯甲酰胺 | PF-429242 | 947303-87-9 | C25H35N3O2 |
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(R)-2-(7-(4-环戊基-3-(三氟甲基)苄氧基)-1,2,3,4-四氢环戊并[b]吲哚-3-基)乙酸 | (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid | 1206123-37-6 | C26H26F3NO3 |
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(R)-(+)-阿替洛尔 | (+)-(R)-atenolol | 56715-13-0 | C14H22N2O3 |
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(R)-(+)-乙莫克舍钠盐 | 828934-41-4 | C15H19ClNaO4 |
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(E)-3-[4-[(E)-2-(2-氯-4-氟苯基)-1-(1H-吲唑-5-基)丁-1-烯-1-基]苯基]-2-丙烯酸 | GDC-0810 | 1365888-06-7 | C26H20ClFN2O2 |
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(E)-3-[3,5-二氟-4-[(1R,3R)-2-(2-氟-2-甲基丙基)-3-甲基-2,3,4,9-四氢-1H-吡啶并[3,4-B]吲哚-1-基]苯基]丙烯酸 | AZD9496 | 1639042-08-2 | C25H25F3N2O2 |
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(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-基)亚苄基]哌啶-2-酮 | (E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]piperidin-2-one | 870843-42-8 | C25H26FN3O2 |
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(DIPHENYLMETHOXY)GBR-12935,1-(2-乙基)-4-(3-苯丙基)哌嗪 | 1-(2-benzhydryloxy-ethyl)-4-(3-phenyl-propyl)-piperazine | 76778-22-8 | C28H34N2O |
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(ALPHAS)-ALPHA-[[[5-(3-甲基-1H-吲唑-5-基)-3-吡啶基]氧基]甲基]-(S)-1H-吲哚-3-乙胺 | (2S)-1-(1H-indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan-2-amine | 552325-16-3 | C24H23N5O |
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(ALPHAS)-3'-氯-ALPHA-[[(1S)-2-乙氧基-1-甲基-2-氧代乙基]氨基][1,1'-联苯]-4-丙酸 | (S)-3-(3'-chlorobiphenyl-4-yl)-2-((S)-1-ethoxycarbonylethylamino)propionic acid | 1308256-94-1 | C20H22ClNO4 |
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(9CI)-5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4(1H,3H)-嘧啶二酮盐酸盐 | 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracil hydrochloride | 183204-72-0 | C9H11ClN4O2*ClH |
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(8S,10S)-8-乙酰基-7,8,9,10-四氢-6,8,11-三羟基-1-甲氧基-10-[[2,3,6-三脱氧-3-[[[[4-(beta-D-吡喃半乳糖基氧基)-3-硝基苯基]甲氧基]羰基]氨基]-alpha-L-来苏-己糖吡喃糖苷]氧基]-5,12-并四苯醌 | [3-Nitro-4-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]methyl N-[(2S,3S,4S,6R)-6-[[(1S,3S)-3-acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-2,4-dihydro-1H-tetracen-1-yl]oxy]-3-hydroxy-2-methyloxan-4-yl]carbamate | 290304-24-4 | C41H44N2O20 |
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(8R,9S)-5-氟-8-(4-氟苯基)-2,7,8,9-四氢-9-(1-甲基-1H-1,2,4-三唑-5-基)-3H-吡啶并[4,3,2-de]酞嗪-3-酮 | (8R,9S)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3 ,2-de] phthalazin-3(7H)-one | 1207456-00-5 | C19H14F2N6O |
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(6aR)-3-异丙基-1-(甲基磺酰基)-4-[(2E)-4-(1-哌啶基)-2-丁烯酰]六氢吡咯并[3,2-b]吡咯-2(1H)-酮盐酸盐(1:1) | Pyrrolo(3,2-b)pyrrol-2(1H)-one, hexahydro-3-(1-methylethyl)-1-(methylsulfonyl)-4-((2E)-1-oxo-4-(1-piperidinyl)-2-butenyl)-, (3S,3aS,6aR)- | 198062-54-3 | C19H31N3O4S |
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