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 |
|---|---|---|---|
| —— | CHIR-090 | 728865-23-4 | C24H27N3O5 |
| —— | [(2-Methyl-4-oxo-5-propan-2-ylcyclohexa-2,5-dien-1-ylidene)amino] 2-methylbenzoate | 321688-88-4 | C18H19NO3 |
| —— | ESI-09 | 263707-16-0 | C16H15ClN4O2 |
| —— | N-[4-[2-(6-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]quinoline-4-carboxamide | 215803-78-4 | C28H30N4O |
| —— | 2-[4-[4-(7-aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexyl]acetic acid | 1031336-60-3 | C20H22N4O2 |
| —— | 9,10-Deepithio-9,10-didehydroacanthifolicin | 78111-17-8 | C44H68O13 |
| —— | 24,25-Dihydroxyvitamine D3 | 40013-87-4 | C27H44O3 |
| —— | Bis[(4-chlorophenyl)methylene]-carbonimidic Dihydrazide | 25875-51-8 | C15H13Cl2N5 |
| —— | 1, Acanthifolicin deriv. | 78111-17-8 | C44H68O13 |
| —— | tenovin-6 | 1011301-29-3 | C25H34N4O2S*ClH |
| —— | (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one monophosphate | 1642303-38-5 | C29H26FN7O*H3O4P |
| —— | Cibinetide | 1208243-50-8 | C51H84N16O21 |
| —— | Unii-1W21G5Q4N2 | 78111-17-8 | C44H68O13 |
| —— | 6-(6-hydroxymethyl pyrimidin-4-yloxy)naphthalene-1-carboxylic acid (3-trifluoromethyl phenyl)amide | 890128-81-1 | C23H16F3N3O3 |
| —— | (2R)-3-[(6R)-2-[(E,2R)-4-[(2'R,8aR)-4-hydroxy-2-[(3S)-1-hydroxy-3-[(2S,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 |
| —— | UK5099 | 56396-35-1 | C18H12N2O2 |
| —— | S-1-(3,6-dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol | 1235481-43-2 | C22H20Br2N2O2 |
| —— | (2R)-3-[(2S,8S,11R)-2-[(E,2R)-4-[(2S,4R,4aS,8aR)-4-hydroxy-2-[(1S,3S)-1-hydroxy-3-[(2S,3R)-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 |
| —— | Cdk2 inhibitor III | 199986-75-9 | C20H28N6O3 |
| —— | Poloxin | 321688-88-4 | C18H19NO3 |
| —— | Carbobenzoxy-valinyl-phenylalaninal | 88191-84-8 | C22H26N2O4 |
| —— | SU 5402 | 215543-92-3 | C17H16N2O3 |
| —— | 1,2,3,4-Tetrahydroacridin-10-ium-9-amine;chloride;hydrate | 206658-92-6 | C13H17ClN2O |
| —— | (2R)-3-[(2S,6R,8S,11R)-2-[(E,2R)-4-[(2S,2'S,4R,4aS,6R,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 |
| —— | substance P | 71977-09-8 | C63H97N17O14S |
| —— | N-(2,6-diethylphenyl)-8-({2-methoxy-4-[(1-methylpiperidin-4-yl)carbamoyl]phenyl}amino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | 1202055-34-2 | C35H42N8O3 |
| —— | CPI-1205 | 1621862-70-1 | C27H33F3N4O3 |
| —— | SA4503 | 165377-44-6 | C23H32N2O2*2ClH |
| —— | 4-(4-fluorophenoxy)benzaldehyde semicarbazone | 181144-66-1 | C14H12FN3O2 |
| —— | PIK-75 | 372196-67-3 | C16H14BrN5O4S |
| —— | XMD 8-85 | 1234479-76-5 | C25H29N7O2 |
| —— | Glykochenodeoxycholsaeure | 640-79-9 | C26H43NO5 |
| —— | Glykochenodesoxycholsaeure | 640-79-9 | C26H43NO5 |
| —— | PF-4136309 | 1341224-83-6 | C29H31F3N6O3 |
| —— | pristinamycin IA | 3131-03-1 | C45H54N8O10 |
| —— | β-(p-fluorophenyl)-γ-aminobutyric acid | 52237-19-1 | C10H12FNO2 |
| —— | PSN632408 | 857652-30-3 | C18H24N4O4 |
| —— | 1-((4'-(cyclopropylmethyl)-2-(pyridin-4-ylamino)-[4,5'-bipyrimidin]-2'-yl)amino)-2-methylpropan-2-ol | 1383716-46-8 | C21H25N7O |
| —— | 1,24,25-trihydroxyvitamin D<sub>3</sub> | 72203-93-1 | C27H44O4 |
| —— | Lobeglitazone sulfate | 763108-62-9 | C24H24N4O5S*H2O4S |
| —— | 6-(2-amino-pyrimidin-4-yloxy)naphthalene-1-carboxylic acid (3-trifluoromethyl phenyl)amide | 861875-60-7 | C22H15F3N4O2 |
| —— | Lonsurf | 733030-01-8 | C19H23Cl2F3N6O7 |
| —— | 1alpha-Hydroxy VD4 | 143032-85-3 | C28H46O2 |
| —— | benzyloxycarbonyl-Val-Ala-Asp-fluoromethylketone | 161401-82-7 | C21H28FN3O7 |
| —— | 3-(4-{1-[2-(4-amino-phenyl)-2-oxo-ethyl]-1H-benzoimidazol-2-yl}-furazan-3-ylamino)-propionitrile | 798577-91-0 | C20H17N7O2 |
| —— | (2R,3S)-3-(cyclopropylmethyl)-N-((3S)-9-fluoro-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2-(3,3,3-trifluoropropyl)succinamide | 1584713-87-0 | C26H26F4N4O3 |
| —— | BMS-345541 | 445430-59-1 | C14H17N5*ClH |
| —— | 3alpha,20alpha-Dihydroxy-5beta-pregnane | 80-92-2 | C21H36O2 |
| —— | ATN-161 | 262438-43-7 | C23H35N9O8S |
| —— | Ceralasertib | 1352226-88-0 | C20H24N6O2S |
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