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。
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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。
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完全激动剂：能够完全激活受体，达到最大生物活性。
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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。
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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。
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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。
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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。
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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 |
|---|---|---|---|---|
| —— | 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 |
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| —— | Sancycline | 808-26-4 | C21H22N2O7 |
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| —— | (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 |
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| —— | Vidofludimus calcium anhydrous | 717824-30-1 | C40H34CaF2N2O8 |
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| —— | (R)-(+)-Etomoxir sodium salt | 828934-41-4 | C15H18ClNaO4 |
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| —— | Lefamulin | 1061337-51-6 | C28H45NO5S |
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| —— | 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 |
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| —— | Potassium O-[(3aR,4R,5S,7R)-octahydro-1H-4,7-methanoinden-5-yl] carbonodithioate | 1096687-52-3 | C11H15KOS2 |
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| —— | Sodium 5-chloro-3-(ethyl(phenyl)carbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate | 248282-07-7 | C19H17ClN2NaO3 |
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| —— | Bavisant (dihydrochloride) | 929622-09-3 | C19H29Cl2N3O2 |
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| —— | 20,25-Diazacholesterol hydrochloride | 1249-84-9 | C25H45ClN2O |
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| —— | Quarfloxin, (R)- | 783361-78-4 | C35H33FN6O3 |
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| —— | Phenylalanyl-leucyl-leucyl-arginyl-asparagine | 141136-84-7 | C31H51N9O7 |
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| —— | 5-Methylcyclocytidine hydrochloride | 51391-96-9 | C10H14ClN3O4 |
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| —— | (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 |
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| —— | MG-132 | 1211877-36-9 | C26H41N3O5 |
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| —— | Varenicline dihydrochloride | 249296-44-4 | C13H15Cl2N3 |
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| —— | (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 |
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| —— | (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 |
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| —— | (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 |
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| —— | Ro 67-7476 | 298690-60-5 | C17H18FNO2S |
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| —— | (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 |
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| —— | Gadolinium-DO3A-butriol | 138071-82-6 | C18H31GdN4O9 |
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| —— | (5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;dihydrochloride | 153504-70-2 | C20H38Cl2N2O3S2 |
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| —— | 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 |
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| —— | But-2-enedioic acid--4-[(1S,2R)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol (1/1) | 169274-78-6 | C26H33NO6 |
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| —— | (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 |
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| —— | PF-543 (Citrate) | 1415562-83-2 | C33H39NO11S |
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| —— | 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 |
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| —— | Tricyclo(3.3.1.13,7)decane-1-carboxamide, 3-(4-chlorophenyl)-N-(4-pyridinylmethyl)- | 915385-81-8 | C23H25ClN2O |
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| —— | (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 |
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| —— | (E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)methylene)pyrazolidine-3,5-dione | 423148-78-1 | C14H7ClFN3O5 |
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| —— | CBB1007 | 1379573-92-8 | C27H34N8O4 |
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| —— | 1-(3-Chloro-4-fluorophenyl)-4-[(5-nitrofuran-2-yl)methylidene]pyrazolidine-3,5-dione | 423148-78-1 | C14H7ClFN3O5 |
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| —— | 4-(1-cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl)pyrimidin-2-amine hydrochloride | 950912-80-8 | C19H20FN5*(x)ClH |
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| —— | (+-)-cis-2-Methylspiro(1,3-oxathiolane-5,3'-quinuclidine) hydrochloride, hemihydrate | 153504-70-2 | C20H38Cl2N2O3S2 |
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| —— | Manganese(2+);3,10,13,20,26-pentazatetracyclo[20.3.1.04,9.014,19]hexacosa-1(26),22,24-triene;chloride | 218791-21-0 | C21H35MnN5*2Cl |
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| —— | trans-(S)-4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9H-purin-2-ylamino]-cyclohexan-1-ol | 899805-25-5 | C21H23F3N6O2 |
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| —— | (2R)-3-[(2S,6R,8S,11R)-2-[(E,2R)-4-[(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-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 |
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| —— | WAY-100635 maleate salt | 634908-75-1 | C29H38N4O6 |
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| —— | α-[2-[4-(3,4-dichlorophenyl)-2-thiazolyl]hydrazinylidene]-2-nitrobenzenepropanoic acid | 315706-13-9 | C18H12Cl2N4O4S |
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| —— | alofanib | 1612888-66-0 | C19H15N3O6S |
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| —— | (5α,20β<sub>F</sub><i>H</i>)-cholestan-3-one | 566-88-1 | C27H46O |
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| —— | (5α)-cholestan-3-one | 566-88-1 | C27H46O |
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| —— | 19-Nor-Δ<sup>4.9</sup>-androstadien-3.17-dion | 5173-46-6 | C18H22O2 |
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| —— | beclabuvir | 958002-33-0 | C36H45N5O5S |
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| —— | (2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid (4-carbamoyl-2-methoxyphenyl)amide | 1309684-94-3 | C31H31Cl2FN4O4 |
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| —— | nortropine | 538-09-0 | C7H13NO |
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| —— | 1H-Pyrrole-3-carboxamide, 5-((5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-N-((2S)-2-hydroxy-3-(4-morpholinyl)propyl)-2,4-dimethyl- | 452105-23-6 | C23H27FN4O4 |
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| —— | estra-4,9-dien-3,17-dione | 5173-46-6 | C18H22O2 |
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