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    首页 分子通 按物质功能分类 生物化工 生化试剂 激动剂抑制剂

    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。

    1. 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。

    2. 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
    —— Pyr6 245747-08-4 C17H9F7N4O
    Pyr6
    —— thiamet-G 1009816-48-1 C9H16N2O4S
    thiamet-G
    —— (8R*,9S*,11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H, 8H, 11H-2, 7b, 11a-triazadibenzo(a,g)cycloocta(cde)trinden-1-one 97161-97-2 C27H21N3O5
    (8R*,9S*,11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H, 8H, 11H-2, 7b, 11a-triazadibenzo(a,g)cycloocta(cde)trinden-1-one
    —— T16Ainh-A01 552309-42-9 C19H20N4O3S2
    T16Ainh-A01
    —— RTA 405 932730-51-3 C33H46N2O3
    RTA 405
    —— 1-(2-methylbenzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea 249889-64-3 C17H13N5O2
    1-(2-methylbenzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
    —— 1-Piperazineacetamide, 4-((3-(7-chloro-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-indol-3-yl)-1,2,4-oxadiazol-5-yl)methyl)- 1050478-18-6 C23H29ClN6O3
    1-Piperazineacetamide, 4-((3-(7-chloro-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-indol-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-
    —— JNJ 39758979 1046447-90-8 C11H19N5
    JNJ 39758979
    —— Posaconazole hydrate 1198769-38-8 C37H44F2N8O5
    Posaconazole hydrate
    —— N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]phenyl]-3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzamide 1604810-84-5 C31H28ClN7O2
    N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]phenyl]-3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
    —— TG-100801 Hydrochloride 1018069-81-2 C33H31Cl2N5O3
    TG-100801 Hydrochloride
    —— (2R)-2-hydroxy-3-[(2S,6R,8S)-11-hydroxy-2-[(E,2R)-4-[(2S,2'S,4R,6R)-4-hydroxy-2-[(3S)-1-hydroxy-3-[(3R,6S)-3-methyl-1,7-dioxaspiro[5.5]undecan-2-yl]butyl]-3-methylidenespiro[4a,7,8,8a-tetrahydro-4H-pyrano[3,2-b]pyran-6,5'-oxolane]-2'-yl]but-3-en-2-yl]-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-methylpropanoic acid 78111-17-8 C44H68O13
    (2R)-2-hydroxy-3-[(2S,6R,8S)-11-hydroxy-2-[(E,2R)-4-[(2S,2'S,4R,6R)-4-hydroxy-2-[(3S)-1-hydroxy-3-[(3R,6S)-3-methyl-1,7-dioxaspiro[5.5]undecan-2-yl]butyl]-3-methylidenespiro[4a,7,8,8a-tetrahydro-4H-pyrano[3,2-b]pyran-6,5'-oxolane]-2'-yl]but-3-en-2-yl]-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-methylpropanoic acid
    —— Pirmavar 61477-94-9 C22H31ClN2O
    Pirmavar
    —— Sodium;6-fluoro-2-[4-(2-fluorophenyl)phenyl]-3-methylquinoline-4-carboxylic acid 96201-88-6 C23H15F2NNaO2+
    Sodium;6-fluoro-2-[4-(2-fluorophenyl)phenyl]-3-methylquinoline-4-carboxylic acid
    —— imino-methyl-[1-[6-(3-methylmorpholin-4-yl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]cyclopropyl]-oxo-lambda6-sulfane 1352226-88-0 C20H24N6O2S
    imino-methyl-[1-[6-(3-methylmorpholin-4-yl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]cyclopropyl]-oxo-lambda6-sulfane
    —— HA 130 1229652-21-4 C24H19BFNO5S
    HA 130
    —— 5-{3-[4-(Aminomethyl)phenoxy]propyl}-2-{(8E)-8-[2-(1,3-benzothiazol-2-yl)hydrazinylidene]-5,6,7,8-tetrahydronaphthalen-2-yl}-1,3-thiazole-4-carboxylic acid 1431866-33-9 C31H29N5O3S2
    5-{3-[4-(Aminomethyl)phenoxy]propyl}-2-{(8E)-8-[2-(1,3-benzothiazol-2-yl)hydrazinylidene]-5,6,7,8-tetrahydronaphthalen-2-yl}-1,3-thiazole-4-carboxylic acid
    —— Cyclohexanol, 4-(4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl)-, trans- 193551-21-2 C20H21FN4O2
    Cyclohexanol, 4-(4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl)-, trans-
    —— N-(3-methoxyphenyl)-4-chlorocinnamanilide 1649486-65-6 C16H14ClNO2
    N-(3-methoxyphenyl)-4-chlorocinnamanilide
    —— Tauroursodeoxycholic acid sodium salt 6009-98-9 C26H44NO6S*Na
    Tauroursodeoxycholic acid sodium salt
    —— CX691 211735-76-1 C12H13N3O2
    CX691
    —— PIM447 1210608-43-7 C24H23F3N4O
    PIM447
    —— 1-(3-(4-cyanophenoxy)phenyl)-3-(4-chloro-3-(trifluoromethyl)phenyl)urea 1400989-25-4 C21H13ClF3N3O2
    1-(3-(4-cyanophenoxy)phenyl)-3-(4-chloro-3-(trifluoromethyl)phenyl)urea
    —— 3-chloro-N-[4-(methylamino)cyclohexyl]-N-[(3-pyridin-4-ylphenyl)methyl]-1-benzothiophene-2-carboxamide 912545-86-9 C28H28ClN3OS
    3-chloro-N-[4-(methylamino)cyclohexyl]-N-[(3-pyridin-4-ylphenyl)methyl]-1-benzothiophene-2-carboxamide
    —— SAR405 1523406-39-4 C19H21ClF3N5O2
    SAR405
    —— Nutlin-3 548472-68-0 C30H30Cl2N4O4
    Nutlin-3
    —— 5-chloro-4-(1H-indol-3-yl)-N-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidin-2-amine 1356962-34-9 C29H34ClN7O
    5-chloro-4-(1H-indol-3-yl)-N-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidin-2-amine
    —— [N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulphonyl}-2-(2-methoxyphenyl)acetamide] 915191-42-3 C32H33N3O7S
    [N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulphonyl}-2-(2-methoxyphenyl)acetamide]
    —— vaniprevir 923590-37-8 C38H55N5O9S
    vaniprevir
    —— H-89 127243-85-0 C20H20BrN3O2S
    H-89
    —— spiculisporic acid 469-77-2 C17H28O6
    spiculisporic acid
    —— (2R)-1-{4-[(1aR,6r,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol 167354-41-8 C32H31F2N3O2
    (2R)-1-{4-[(1aR,6r,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol
    —— 6-((1R,2S)-2-amino-cyclohexylamino)-4-(5,6-dimethyl-pyridin-2-ylamino)-pyridazine-3-carboxylic acid amide 1446790-62-0 C18H25N7O
    6-((1R,2S)-2-amino-cyclohexylamino)-4-(5,6-dimethyl-pyridin-2-ylamino)-pyridazine-3-carboxylic acid amide
    —— Y-27632 dihydrochloride 146986-50-7 C14H21N3O
    Y-27632 dihydrochloride
    —— bleomycin 11056-06-7 C55H84N17O21S3
    bleomycin
    —— 3-methyl-2-((1S,2S)-2-(quinolin-2-yl)cyclopropyl)-3H-imidazo[4,5-f]quinoline 1516896-09-5 C21H19N7
    3-methyl-2-((1S,2S)-2-(quinolin-2-yl)cyclopropyl)-3H-imidazo[4,5-f]quinoline
    —— 5-(4-methoxy-<i>trans</i>-cinnamylidene)-barbituric acid 100872-83-1 C14H12N2O4
    5-(4-methoxy-<i>trans</i>-cinnamylidene)-barbituric acid
    —— (E)-3-(2,4-dimethoxybenzylidene)-3,4,5,6-tetra-hydro-2,3'-bipyridine dihydrochloride 156223-05-1 C19H20N2O2*2ClH
    (E)-3-(2,4-dimethoxybenzylidene)-3,4,5,6-tetra-hydro-2,3'-bipyridine dihydrochloride
    —— 4(3H)-Quinazolinone, 3-(2-chlorophenyl)-2-(2-(6-((diethylamino)methyl)-2-pyridinyl)ethenyl)-6-fluoro- 199655-36-2 C26H24ClFN4O
    4(3H)-Quinazolinone, 3-(2-chlorophenyl)-2-(2-(6-((diethylamino)methyl)-2-pyridinyl)ethenyl)-6-fluoro-
    —— (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide 1223498-69-8 C18H21F3N4O3S
    (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide
    —— DDD00175799 100872-83-1 C14H12N2O4
    DDD00175799
    —— N-1R-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl-N-pyridin-3-ylmethyl-2-(4-trifluoromethoxyphenyl)-acetamide 473719-41-4 C32H28F3N5O4
    N-1R-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl-N-pyridin-3-ylmethyl-2-(4-trifluoromethoxyphenyl)-acetamide
    —— gold(1+);3,4,5-trihydroxy-6-(hydroxymethyl)oxane-2-thiolate 12192-57-3 C6H11AuO5S
    gold(1+);3,4,5-trihydroxy-6-(hydroxymethyl)oxane-2-thiolate
    —— N2-[(1S)-1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine 1239358-86-1 C21H20FN7
    N2-[(1S)-1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine
    —— zosuquidar 167465-36-3 C32H31F2N3O2
    zosuquidar
    —— 2-[Bis[2-[carboxymethyl-[2-(methylamino)-2-oxoethyl]amino]ethyl]amino]acetic acid;gadolinium 131410-48-5 C16H29GdN5O8
    2-[Bis[2-[carboxymethyl-[2-(methylamino)-2-oxoethyl]amino]ethyl]amino]acetic acid;gadolinium
    —— K-Ras G12C-IN-3 1629268-19-4 C21H19Cl3N2O3
    K-Ras G12C-IN-3
    —— sequella 502487-67-4 C22H38N2
    sequella
    —— cenicriviroc 497223-25-3 C41H52N4O4S
    cenicriviroc
    —— potassium O-((3aR,4R,5S,7R,7aR)-octahydro-1H-4,7-methanoinden-5-yl) carbonodithioate 473281-59-3 C11H15OS2*K
    potassium O-((3aR,4R,5S,7R,7aR)-octahydro-1H-4,7-methanoinden-5-yl) carbonodithioate