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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
    —— tandospirone citrate 112457-95-1 C6H8O7*C21H29N5O2
    tandospirone citrate
    —— sodium tauroursodeoxycholate 35807-85-3 C26H44NO6S*Na
    sodium tauroursodeoxycholate
    —— methylprednisolone sodium succinate 2375-03-3 C26H33O8*Na
    methylprednisolone sodium succinate
    —— (4E)-4-(Hydroxyimino)-2-isopropyl-5-methyl-2,5-cyclohexadien-1-on e 17302-61-3 C10H13NO2
    (4E)-4-(Hydroxyimino)-2-isopropyl-5-methyl-2,5-cyclohexadien-1-on e
    —— Nortropine 538-09-0 C7H13NO
    Nortropine
    —— {(2R)-2-[4-(4-{2-[(methylsulfonyl)amino]ethyl}phenyl)phenyl]-propyl}[(methylethyl)sulfonyl]amine 375345-95-2 C21H30N2O4S2
    {(2R)-2-[4-(4-{2-[(methylsulfonyl)amino]ethyl}phenyl)phenyl]-propyl}[(methylethyl)sulfonyl]amine
    —— Mc-Val-Cit-PAB-MMAE 646502-53-6 C68H105N11O15
    Mc-Val-Cit-PAB-MMAE
    —— 2-(3-(6-(2-(2,4-dichlorophenyl)ethylamino)-2-methoxy-pyrimidin-4-yl)phenyl)-2-methyl-propionic acid 885066-67-1 C23H23Cl2N3O3
    2-(3-(6-(2-(2,4-dichlorophenyl)ethylamino)-2-methoxy-pyrimidin-4-yl)phenyl)-2-methyl-propionic acid
    —— OSU-T315 1333146-24-9 C30H30F3N5O
    OSU-T315
    —— sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] 197723-00-5 C14H12Cl4N4Ru*Na
    sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)]
    —— NAEPA 24435-25-4 C20H40NO5P
    NAEPA
    —— Fagomin 53185-12-9 C6H13NO3
    Fagomin
    —— Pregnandiol 80-89-7 C21H36O2
    Pregnandiol
    —— 1,4,5,6,8-Pentaazaacenaphthylen-3-amine 61966-08-3 C13H17N6O7P
    1,4,5,6,8-Pentaazaacenaphthylen-3-amine
    —— Eltrombopag 496775-61-2 C25H22N4O4
    Eltrombopag
    —— Behenoyl-arabinofuranosyl-cytosine 55726-47-1 C31H55N3O6
    Behenoyl-arabinofuranosyl-cytosine
    —— 4-amino-1-(2-hydroxymethyl-[1,3]dioxolan-4-yl)-1H-pyrimidin-2-one 145918-75-8 C8H11N3O4
    4-amino-1-(2-hydroxymethyl-[1,3]dioxolan-4-yl)-1H-pyrimidin-2-one
    —— 2-hydroxy-3-[11-hydroxy-2-[4-[4-hydroxy-2-[1-hydroxy-3-(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
    2-hydroxy-3-[11-hydroxy-2-[4-[4-hydroxy-2-[1-hydroxy-3-(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
    —— sobetirome 211110-63-3 C20H24O4
    sobetirome
    —— cholestan-3-one 566-88-1 C27H46O
    cholestan-3-one
    —— [13,20,22-Trihydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3-oxo-19-(prop-2-enylamino)-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18(22),19-hexaen-9-yl] carbamate 857402-23-4 C31H45N3O8
    [13,20,22-Trihydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3-oxo-19-(prop-2-enylamino)-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18(22),19-hexaen-9-yl] carbamate
    —— isoindigo 476-34-6 C16H10N2O2
    isoindigo
    —— 1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]-N-methylpyrazole-4-carboxamide 313348-27-5 C15H18N8O5
    1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]-N-methylpyrazole-4-carboxamide
    —— 5-[2-[1-(5,6-dimethylhept-3-en-2-yl)-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol 54573-75-0 C28H44O2
    5-[2-[1-(5,6-dimethylhept-3-en-2-yl)-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
    —— 4-Amino-1-[3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodopyrimidin-2-one 69123-90-6 C9H11FIN3O4
    4-Amino-1-[3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodopyrimidin-2-one
    —— [(8R,9S,10R,13S,14S,17R)-17-acetyl-13-methyl-16-methylidene-3-oxo-2,6,7,8,9,10,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate 7759-35-5 C23H30O4
    [(8R,9S,10R,13S,14S,17R)-17-acetyl-13-methyl-16-methylidene-3-oxo-2,6,7,8,9,10,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate
    —— milnacipran 136090-84-1 C15H22N2O
    milnacipran
    —— [5-(6-Aminopurin-9-yl)-4-fluorooxolan-2-yl]methanol 110143-10-7 C10H12FN5O2
    [5-(6-Aminopurin-9-yl)-4-fluorooxolan-2-yl]methanol
    —— Breviscapine 116122-36-2 C21H18O12
    Breviscapine
    —— 4-[[3,3-dimethyl-2-[[3-methyl-2-(methylamino)-3-phenylbutanoyl]amino]butanoyl]-methylamino]-2,5-dimethylhex-2-enoic acid 228266-40-8 C27H43N3O4
    4-[[3,3-dimethyl-2-[[3-methyl-2-(methylamino)-3-phenylbutanoyl]amino]butanoyl]-methylamino]-2,5-dimethylhex-2-enoic acid
    —— rac-Estra-4,9-diene-3,17-dione 5173-46-6 C18H22O2
    rac-Estra-4,9-diene-3,17-dione