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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
    —— Avermectin A1a, 25-cyclohexyl-4'-O-de(2,6-dideoxy-3-O-methyl--L-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)- 165108-07-6 C43H63NO11
    Avermectin A1a, 25-cyclohexyl-4'-O-de(2,6-dideoxy-3-O-methyl--L-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)-
    —— benzyl N-[(2R)-3-methyl-1-oxo-1-[[(2R)-1-oxo-3-phenylpropan-2-yl]amino]butan-2-yl]carbamate 88191-84-8 C22H26N2O4
    benzyl N-[(2R)-3-methyl-1-oxo-1-[[(2R)-1-oxo-3-phenylpropan-2-yl]amino]butan-2-yl]carbamate
    —— 1-[(Z)-(4-chlorophenyl)methylideneamino]-2-[(E)-(4-chlorophenyl)methylideneamino]guanidine 25875-51-8 C15H13Cl2N5
    1-[(Z)-(4-chlorophenyl)methylideneamino]-2-[(E)-(4-chlorophenyl)methylideneamino]guanidine
    —— GSK525768A 1260530-25-3 C22H22ClN5O2
    GSK525768A
    —— Syk Inhibitor IV, BAY 61-3606 648903-57-5 C20H19ClN6O3
    Syk Inhibitor IV, BAY 61-3606
    —— [(3~{S},4~{S})-3-methoxyoxan-4-yl]-[(1~{R},3~{S})-3-propan-2-yl-3-[[3-(trifluoromethyl)-7,8-dihydro-5~{H}-1,6-naphthyridin-6-yl]carbonyl]cyclopentyl]azanium 624733-88-6 C24H35F3N3O3+
    [(3~{S},4~{S})-3-methoxyoxan-4-yl]-[(1~{R},3~{S})-3-propan-2-yl-3-[[3-(trifluoromethyl)-7,8-dihydro-5~{H}-1,6-naphthyridin-6-yl]carbonyl]cyclopentyl]azanium
    —— P-P-Ura-LRibf.2Na+ 27821-45-0 C9H12N2Na2O12P2
    P-P-Ura-LRibf.2Na+
    —— GSK-3117391 1018673-42-1 C22H33N3O4
    GSK-3117391
    —— Pharmakon1600-01503255 2375-03-3 C26H34NaO8+
    Pharmakon1600-01503255
    —— Ethanone, 1-(7,8-dihydro-2-((9-(trans-4-methylcyclohexyl)-9H-pyrido(4',3':4,5)pyrrolo(2,3-d)pyrimidin-2-yl)amino)-1,6-naphthyridin-6(5H)-yl)-2-hydroxy- 1401033-86-0 C26H29N7O2
    Ethanone, 1-(7,8-dihydro-2-((9-(trans-4-methylcyclohexyl)-9H-pyrido(4',3':4,5)pyrrolo(2,3-d)pyrimidin-2-yl)amino)-1,6-naphthyridin-6(5H)-yl)-2-hydroxy-
    —— (Thiene-2,5-diyl)bis(methylene) dicarbamimidothioate--hydrogen chloride (1/1) 2076-91-7 C8H13ClN4S3
    (Thiene-2,5-diyl)bis(methylene) dicarbamimidothioate--hydrogen chloride (1/1)
    —— L-Valinamide,N-dimethyl-L-valyl-N-[2-methoxy-4-[2-[1-methoxy-2-methyl-3-oxo-3-[[2-phenyl-1-(2-thiazolyl)ethyl] amino]propyl]-1-pyrrolidinyl]-1-(1-methylpropyl)-4-oxobutyl]-N-methyl-, [2S-[1[1R*(R*),2S*],2R*[1S*,2S*,3(R*)]]]- 110417-88-4 C42H68N6O6S
    L-Valinamide,N-dimethyl-L-valyl-N-[2-methoxy-4-[2-[1-methoxy-2-methyl-3-oxo-3-[[2-phenyl-1-(2-thiazolyl)ethyl] amino]propyl]-1-pyrrolidinyl]-1-(1-methylpropyl)-4-oxobutyl]-N-methyl-, [2S-[1[1R*(R*),2S*],2R*[1S*,2S*,3(R*)]]]-
    —— Blenoxane (TN) (Bristol Meyers) 9041-93-4 C55H85N17O25S4
    Blenoxane (TN) (Bristol Meyers)
    —— Sancycline 808-26-4 C21H22N2O7
    Sancycline
    —— (2R,3R,4S,5S,6R)-2-[[(2R,3S,4S,5R,6R)-6-[[(3S,8R,9R,10S,11R,13R,14S,17R)-17-[(2R,5R)-5-[(2S,3R,4S,5S,6R)-4,5-dihydroxy-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-[[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl]oxy-6-hydroxy-6-methylheptan-2-yl]-11-hydroxy-4,4,9,13,14-pentamethyl-2,3,7,8,10,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]-3,4-dihydroxy-5-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]methoxy]-6-(hydroxymethyl)oxane-3,4,5-triol 89590-98-7 C66H112O34
    (2R,3R,4S,5S,6R)-2-[[(2R,3S,4S,5R,6R)-6-[[(3S,8R,9R,10S,11R,13R,14S,17R)-17-[(2R,5R)-5-[(2S,3R,4S,5S,6R)-4,5-dihydroxy-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-[[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl]oxy-6-hydroxy-6-methylheptan-2-yl]-11-hydroxy-4,4,9,13,14-pentamethyl-2,3,7,8,10,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]-3,4-dihydroxy-5-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]methoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
    —— Vidofludimus calcium anhydrous 717824-30-1 C40H34CaF2N2O8
    Vidofludimus calcium anhydrous
    —— (R)-(+)-Etomoxir sodium salt 828934-41-4 C15H18ClNaO4
    (R)-(+)-Etomoxir sodium salt
    —— Lefamulin 1061337-51-6 C28H45NO5S
    Lefamulin
    —— 3-Acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 2,3,6-trideoxy-3-[({[4-(beta-D-galactopyranosyloxy)-3-nitrophenyl]methoxy}carbonyl)amino]-alpha-L-lyxo-hexopyranoside 290304-24-4 C41H44N2O20
    3-Acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 2,3,6-trideoxy-3-[({[4-(beta-D-galactopyranosyloxy)-3-nitrophenyl]methoxy}carbonyl)amino]-alpha-L-lyxo-hexopyranoside
    —— Potassium O-[(3aR,4R,5S,7R)-octahydro-1H-4,7-methanoinden-5-yl] carbonodithioate 1096687-52-3 C11H15KOS2
    Potassium O-[(3aR,4R,5S,7R)-octahydro-1H-4,7-methanoinden-5-yl] carbonodithioate
    —— Sodium 5-chloro-3-(ethyl(phenyl)carbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate 248282-07-7 C19H17ClN2NaO3
    Sodium 5-chloro-3-(ethyl(phenyl)carbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate
    —— Bavisant (dihydrochloride) 929622-09-3 C19H29Cl2N3O2
    Bavisant (dihydrochloride)
    —— CC-115 hydrochloride 1300118-55-1 C16H17ClN8O
    CC-115 hydrochloride
    —— 20,25-Diazacholesterol hydrochloride 1249-84-9 C25H45ClN2O
    20,25-Diazacholesterol hydrochloride
    —— RGX-104 610318-03-1 C34H33ClF3NO3*ClH
    RGX-104
    —— Quarfloxin, (R)- 783361-78-4 C35H33FN6O3
    Quarfloxin, (R)-
    —— Phenylalanyl-leucyl-leucyl-arginyl-asparagine 141136-84-7 C31H51N9O7
    Phenylalanyl-leucyl-leucyl-arginyl-asparagine
    —— 5-Methylcyclocytidine hydrochloride 51391-96-9 C10H14ClN3O4
    5-Methylcyclocytidine hydrochloride
    —— (2R)-3-[(2S,8S)-2-[(E)-4-[(2S,2'R,4aS,6R,8aR)-4-hydroxy-2-[1-hydroxy-3-[(2S)-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]-11-hydroxy-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-hydroxy-2-methylpropanoic acid 78111-17-8 C44H68O13
    (2R)-3-[(2S,8S)-2-[(E)-4-[(2S,2'R,4aS,6R,8aR)-4-hydroxy-2-[1-hydroxy-3-[(2S)-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]-11-hydroxy-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-hydroxy-2-methylpropanoic acid
    —— 1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid 1193383-09-3 C12H6ClF3N4O3
    1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid
    —— MG-132 1211877-36-9 C26H41N3O5
    MG-132
    —— Sonidegib Phosphate 1218778-77-8 C26H32F3N3O11P2
    Sonidegib Phosphate
    —— Varenicline dihydrochloride 249296-44-4 C13H15Cl2N3
    Varenicline dihydrochloride
    —— (2R)-3-[(2R,6R,8S,11R)-2-[(E,2R)-4-[(2S,2'R,4R,4aS,6S,8aR)-4-hydroxy-2-[(1S,3S)-1-hydroxy-3-[(2S,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]-11-hydroxy-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-hydroxy-2-methylpropanoic acid 78111-17-8 C44H68O13
    (2R)-3-[(2R,6R,8S,11R)-2-[(E,2R)-4-[(2S,2'R,4R,4aS,6S,8aR)-4-hydroxy-2-[(1S,3S)-1-hydroxy-3-[(2S,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]-11-hydroxy-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-hydroxy-2-methylpropanoic acid
    —— Prexasertib dihydrochloride 1234015-54-3 C18H21Cl2N7O2
    Prexasertib dihydrochloride
    —— 1-(1-[(2S)-2-hydroxypropanoyl]piperidin-4-yl)-3-methyl-8-(6-methylpyridin-3-yl)-1,3-dihydro-2H-imidazo[4,5-c][1,5]naphthyridin-2-one 1220699-06-8 C24H26N6O3
    1-(1-[(2S)-2-hydroxypropanoyl]piperidin-4-yl)-3-methyl-8-(6-methylpyridin-3-yl)-1,3-dihydro-2H-imidazo[4,5-c][1,5]naphthyridin-2-one
    —— (2R)-3-[(2S,6R,8S,11R)-2-[(E,1R)-3-[(2S,2'R,4R,6R,8aR)-4-hydroxy-2-[(1S,3S)-1-hydroxy-3-[(3R,6S)-3-methyl-1,7-dioxaspiro[5.5]undecan-2-yl]butyl]-3-methylene-spiro[4a,7,8,8a-tetrahydro-4H-pyrano[3,2-b]pyran-6,5'-tetrahydrofuran]-2'-yl]-1-methyl-allyl]-11-hydroxy-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-hydroxy-2-methyl-propanoic acid 78111-17-8 C44H68O13
    (2R)-3-[(2S,6R,8S,11R)-2-[(E,1R)-3-[(2S,2'R,4R,6R,8aR)-4-hydroxy-2-[(1S,3S)-1-hydroxy-3-[(3R,6S)-3-methyl-1,7-dioxaspiro[5.5]undecan-2-yl]butyl]-3-methylene-spiro[4a,7,8,8a-tetrahydro-4H-pyrano[3,2-b]pyran-6,5'-tetrahydrofuran]-2'-yl]-1-methyl-allyl]-11-hydroxy-4-methyl-1,7-dioxaspiro[5.5]undec-4-en-8-yl]-2-hydroxy-2-methyl-propanoic acid
    —— (1-(3,4-difluorobenzyl)-2-oxo-N-{1(R)-2-[(2-oxo2,3-dihydro-1H-benzimidazol-5-yl)oxy]-1-phenylethyl}-1,2-dihydropyridine-3-carboxamide) 1001409-50-2 C28H22F2N4O4
    (1-(3,4-difluorobenzyl)-2-oxo-N-{1(R)-2-[(2-oxo2,3-dihydro-1H-benzimidazol-5-yl)oxy]-1-phenylethyl}-1,2-dihydropyridine-3-carboxamide)
    —— Ro 67-7476 298690-60-5 C17H18FNO2S
    Ro 67-7476
    —— (2R)-2-hydroxy-3-[(6R)-11-hydroxy-2-[4-[(6R)-4-hydroxy-2-[1-hydroxy-3-[(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-[(6R)-11-hydroxy-2-[4-[(6R)-4-hydroxy-2-[1-hydroxy-3-[(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
    —— Gadolinium-DO3A-butriol 138071-82-6 C18H31GdN4O9
    Gadolinium-DO3A-butriol
    —— (5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;dihydrochloride 153504-70-2 C20H38Cl2N2O3S2
    (5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;dihydrochloride
    —— methyl N-[(2R)-1-[2-[(2S,3S)-2-hydroxy-3-[[(2R)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate 1192224-24-0 C26H43N5O7
    methyl N-[(2R)-1-[2-[(2S,3S)-2-hydroxy-3-[[(2R)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
    —— But-2-enedioic acid--4-[(1S,2R)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol (1/1) 169274-78-6 C26H33NO6
    But-2-enedioic acid--4-[(1S,2R)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol (1/1)
    —— (1R,3S,5Z)-5-[(2E)-2-[(1R,7Ar)-1-[(2R)-5-cyclopropyl-5-hydroxypentan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol 129831-99-8 C27H42O3
    (1R,3S,5Z)-5-[(2E)-2-[(1R,7Ar)-1-[(2R)-5-cyclopropyl-5-hydroxypentan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
    —— PF-543 (Citrate) 1415562-83-2 C33H39NO11S
    PF-543 (Citrate)
    —— (1aR,5S,8S,10R,22aR)-N-[(R-1R,2S)-1-[(cyclopropylsulfonamido)carbonyl]-2-ethenylcyclopropyl]-14-methoxy-5-(2-methylpropan-2-yl)-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide hydrate 1350462-55-3 C38H50N6O9S*H2O
    (1aR,5S,8S,10R,22aR)-N-[(R-1R,2S)-1-[(cyclopropylsulfonamido)carbonyl]-2-ethenylcyclopropyl]-14-methoxy-5-(2-methylpropan-2-yl)-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide hydrate
    —— D-Erythro-pentitol, 1,5-anhydro-2,3-dideoxy-3-(((1R,3S)-3-((7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl)carbonyl)-3-(1-methylethyl)cyclopentyl)amino)-4-o-methyl- 624733-88-6 C24H36F3N3O2
    D-Erythro-pentitol, 1,5-anhydro-2,3-dideoxy-3-(((1R,3S)-3-((7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl)carbonyl)-3-(1-methylethyl)cyclopentyl)amino)-4-o-methyl-
    —— Tricyclo(3.3.1.13,7)decane-1-carboxamide, 3-(4-chlorophenyl)-N-(4-pyridinylmethyl)- 915385-81-8 C23H25ClN2O
    Tricyclo(3.3.1.13,7)decane-1-carboxamide, 3-(4-chlorophenyl)-N-(4-pyridinylmethyl)-
    —— (2S,3R,4R)[[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl ]methyl]-1-oxo-3-phenylpropyl]-amino]acetic acid dihydrate 170098-38-1 C25H32N2O4*2H2O
    (2S,3R,4R)[[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl ]methyl]-1-oxo-3-phenylpropyl]-amino]acetic acid dihydrate