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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
    —— (4-cyclopropylpiperazin-1-yl)(4-(morpholinomethyl)phenyl)methanone dihydrochloride 929622-09-3 C19H27N3O2*2ClH
    (4-cyclopropylpiperazin-1-yl)(4-(morpholinomethyl)phenyl)methanone dihydrochloride
    —— (5α)-pregnane-3β,20α<sub>F</sub>-diol 80-89-7 C21H36O2
    (5α)-pregnane-3β,20α<sub>F</sub>-diol
    —— 3-({[(3R,5R)-3-butyl-3-ethyl-7-(methyloxy)-1,1-dioxo-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepin-8-yl]methyl}amino)pentanedioic acid 1345982-69-5 C28H38N2O7S
    3-({[(3R,5R)-3-butyl-3-ethyl-7-(methyloxy)-1,1-dioxo-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepin-8-yl]methyl}amino)pentanedioic acid
    —— Pregnanediol V 80-89-7 C21H36O2
    Pregnanediol V
    —— (5α)-pregnane-3α,20α<sub>F</sub>-diol 80-89-7 C21H36O2
    (5α)-pregnane-3α,20α<sub>F</sub>-diol
    —— N-(8-{[(2R)-2-hydroxy-3-(morpholin-4-yl)propyl]oxy}-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylpyridine-3-carboxamide 1375469-38-7 C25H30N6O5
    N-(8-{[(2R)-2-hydroxy-3-(morpholin-4-yl)propyl]oxy}-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylpyridine-3-carboxamide
    —— tenapanor 1234423-95-0 C50H66Cl4N8O10S2
    tenapanor
    —— Belizatinib 1357920-84-3 C33H44FN5O3
    Belizatinib
    —— JNJ-28312141 885692-52-4 C26H32N6O2
    JNJ-28312141
    —— (Z)-2-(3,4-dimethoxy-phenyl)-3-[5-(4-hydroxy-piperidin-1-yl)-thiophen-2-yl]-acrylonitrile 912287-56-0 C20H22N2O3S
    (Z)-2-(3,4-dimethoxy-phenyl)-3-[5-(4-hydroxy-piperidin-1-yl)-thiophen-2-yl]-acrylonitrile
    —— bleomycin B1 11056-06-7 C50H73N17O21S2
    bleomycin B1
    —— MK-0773 606101-58-0 C27H34FN5O2
    MK-0773
    —— KNK437 218924-25-5 C13H11NO4
    KNK437
    —— 2-amino-9-(2-deoxy-pentofuranosyl)-1,9-dihydro-purine-6-thione 789-61-7 C10H13N5O3S
    2-amino-9-(2-deoxy-pentofuranosyl)-1,9-dihydro-purine-6-thione
    —— avibactam 1192491-61-4 C7H10N3O6S*Na
    avibactam
    —— evobrutinib 1415823-73-2 C25H27N5O2
    evobrutinib
    —— ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)-[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine succinate 851916-42-2 C4H6O4*C24H34F3N3O3
    ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)-[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine succinate
    —— sutezolid 168828-58-8 C16H20FN3O3S
    sutezolid
    —— telratolimod 1359993-59-1 C36H59N5O2
    telratolimod
    —— GSK-3326595 1616392-22-3 C24H32N6O3
    GSK-3326595
    —— elbasvir 1370468-36-2 C49H55N9O7
    elbasvir
    —— 1,4-bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-enyl)-1,4-diazepane 191089-59-5 C33H48N2O6
    1,4-bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-enyl)-1,4-diazepane
    —— osilodrostat 928134-65-0 C13H10FN3
    osilodrostat
    —— (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide 1443763-60-7 C29H26FN5O4S
    (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide
    —— (1aR,12bS)-8-cyclohexyl-N-[(dimethylamino)sulfonyl]-1,1a,2,12b-tetrahydro-11-methoxy-1a-[(3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl]-cycloprop[d]indolo[2,1-a][2]benzazepine-5-carboxamide 958002-33-0 C36H45N5O5S
    (1aR,12bS)-8-cyclohexyl-N-[(dimethylamino)sulfonyl]-1,1a,2,12b-tetrahydro-11-methoxy-1a-[(3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl]-cycloprop[d]indolo[2,1-a][2]benzazepine-5-carboxamide
    —— Δ<sup>1</sup>-Dehydrotestololacton 968-93-4 C19H24O3
    Δ<sup>1</sup>-Dehydrotestololacton
    —— MK-6096 1088991-73-4 C24H25FN4O2
    MK-6096
    —— 3-[(3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione 1265965-22-7 C22H22N4O4S
    3-[(3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione
    —— DBPR108 1186426-66-3 C16H25FN4O2
    DBPR108
    —— hexadecyloxypropyl-cidofovir 444805-28-1 C27H52N3O7P
    hexadecyloxypropyl-cidofovir
    —— DY 131 95167-41-2 C18H21N3O2
    DY 131
    —— potassium canrenoate 2181-04-6 C22H29O4*K
    potassium canrenoate
    —— Eliglustat Tartrate 928659-70-5 C50H78N4O14
    Eliglustat Tartrate
    —— (+/-)-YS-49 132836-42-1 C20H19NO2
    (+/-)-YS-49
    —— 6-ethyl-N-[1-(hydroxyacetyl)piperidin-4-yl]-1-methyl-4-oxo-5-(2-oxo-2-phenylethyl)-3-(2,2,2-trifluoroethoxy)-4,5-dihydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 1186231-83-3 C28H31F3N4O6
    6-ethyl-N-[1-(hydroxyacetyl)piperidin-4-yl]-1-methyl-4-oxo-5-(2-oxo-2-phenylethyl)-3-(2,2,2-trifluoroethoxy)-4,5-dihydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide
    —— Pf-04447943 1082744-20-4 C20H25N7O2
    Pf-04447943
    —— (2Z,5Z)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one;chloride 147366-41-4 C21H22ClN3OS2
    (2Z,5Z)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one;chloride
    —— (5E)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one;chloride 1427472-75-0 C21H22ClN3OS2
    (5E)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one;chloride
    —— RO-4917523 802906-73-6 C18H13ClFN3
    RO-4917523
    —— Tanzisertib 899805-25-5 C21H23F3N6O2
    Tanzisertib
    —— N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide 1474110-21-8 C25H35NO5S
    N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide
    —— Tesevatinib 781613-23-8 C24H25Cl2FN4O2
    Tesevatinib
    —— N-(2-{[[(2E)-3-(4-chlorophenyl)prop-2-enyl](methyl)amino]methyl}phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide 139298-40-1 C26H29ClN2O4S
    N-(2-{[[(2E)-3-(4-chlorophenyl)prop-2-enyl](methyl)amino]methyl}phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide
    —— angelicin 151823-14-2 C11H6O3
    angelicin
    —— (trans)-2-(2-{2-[2-(4-trifluoromethylphenyl)vinyl]-1H-benzimidazol-5-yl}phenyl)propan-2-ol 956274-94-5 C25H21F3N2O
    (trans)-2-(2-{2-[2-(4-trifluoromethylphenyl)vinyl]-1H-benzimidazol-5-yl}phenyl)propan-2-ol
    —— (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3S,4S,5R)-3-methoxy-1-[(2S)-2-[(1S,2S)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide 110417-88-4 C42H68N6O6S
    (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3S,4S,5R)-3-methoxy-1-[(2S)-2-[(1S,2S)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide
    —— 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one HCl salt 1448754-43-5 C21H16F3N3O3*ClH
    4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one HCl salt
    —— (9H-fluoren-9-yl)methyl ((S)-3-methyl-1-(((S)-1-((4-((((4-nitrophenoxy)carbonyl)oxy)methyl)phenyl)amino)-1-oxo-5-ureidopentan-2-yl)amino)-1-oxobutan-2-yl)carbamate 863971-53-3 C40H42N6O10
    (9H-fluoren-9-yl)methyl ((S)-3-methyl-1-(((S)-1-((4-((((4-nitrophenoxy)carbonyl)oxy)methyl)phenyl)amino)-1-oxo-5-ureidopentan-2-yl)amino)-1-oxobutan-2-yl)carbamate
    —— 6,7-dimethoxy-4-phenylaminoquinazoline 21561-09-1 C16H15N3O2
    6,7-dimethoxy-4-phenylaminoquinazoline
    —— 5α-cholestan-3-one 566-88-1 C27H46O
    5α-cholestan-3-one