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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
(2E)-3-(3-氯苯基)-N-[2-[甲基(四氢-1,1-二氧代-2H-噻喃-4-基)氨基]-2-氧代乙基]-2-丙烯酰胺 ML264 1550008-55-3 C17H21ClN2O4S
(2E)-3-(3-氯苯基)-N-[2-[甲基(四氢-1,1-二氧代-2H-噻喃-4-基)氨基]-2-氧代乙基]-2-丙烯酰胺
(2E)-2-氰基-3-(3,4-二羟基苯基)-N-苯基-2-丙烯酰胺 α-cyano-(3,4-dihydroxy)-N-phenylcinnamide 133550-35-3 C16H12N2O3
(2E)-2-氰基-3-(3,4-二羟基苯基)-N-苯基-2-丙烯酰胺
(2-羟苯基)(吡咯烷-1-基)甲硫酮 o-hydroxythiobenzopyrrolidide 84783-01-7 C11H13NOS
(2-羟苯基)(吡咯烷-1-基)甲硫酮
(1S)-6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺 (1S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide 848193-68-0 C13H13ClN2O
(1S)-6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺
(1S)-2-苯基-1-(1,3-噻唑-2-基)乙胺盐酸盐 Doe hydrochloride 135383-60-7 C11H12N2S*ClH
(1S)-2-苯基-1-(1,3-噻唑-2-基)乙胺盐酸盐
(1S)-1-(4-氯苯基)-1,4-二氢-6-甲氧基-7-(1-甲基乙氧基)-2-[4-[甲基[[反式-4-(4-甲基-3-氧代-1-哌嗪基)环己基]甲基]氨基]苯基]-3(2H)-异喹啉酮 Nvp-cgm097 1313363-54-0 C38H47ClN4O4
(1S)-1-(4-氯苯基)-1,4-二氢-6-甲氧基-7-(1-甲基乙氧基)-2-[4-[甲基[[反式-4-(4-甲基-3-氧代-1-哌嗪基)环己基]甲基]氨基]苯基]-3(2H)-异喹啉酮
(1S)-1,5-脱水-1-C-[4-氯-3-[[4-[2-(环丙氧基)乙氧基]苯基]甲基]苯基]-D-山梨醇 bexagliflozin 1118567-05-7 C24H29ClO7
(1S)-1,5-脱水-1-C-[4-氯-3-[[4-[2-(环丙氧基)乙氧基]苯基]甲基]苯基]-D-山梨醇
(1R,2S)-2-环己基-1-(4-(环丙基磺酰基)苯基)-N-(5-((2-(吡咯烷-1-基)乙基)硫代)噻唑-2-基)环丙烷羧酰胺 LY2608204 1234703-40-2 C28H37N3O3S3
(1R,2S)-2-环己基-1-(4-(环丙基磺酰基)苯基)-N-(5-((2-(吡咯烷-1-基)乙基)硫代)噻唑-2-基)环丙烷羧酰胺
(1R,2R,3S,3AR,8BS)-6-[[(2S,3R,6R)-6-[(1R)-1,2-二羟基乙基]-3-甲氧基-1,4-二氧己环-2-基]氧基]-2,3,3A,8B-四氢-1,8B-二羟基-8-甲氧基-3A-(4-甲氧基苯基)-3-苯基-1H-环戊烯并[B]苯并呋喃-2-羧酸甲酯 (1R,2R,3S,3aR,8bS)-methyl 6-(((2S,3R,6R)-6-((R)-1,2-dihydroxyethyl)-3-methoxy-1,4-dioxan-2-yl)oxy)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-2-carboxylate 697235-38-4 C34H38O13
(1R,2R,3S,3AR,8BS)-6-[[(2S,3R,6R)-6-[(1R)-1,2-二羟基乙基]-3-甲氧基-1,4-二氧己环-2-基]氧基]-2,3,3A,8B-四氢-1,8B-二羟基-8-甲氧基-3A-(4-甲氧基苯基)-3-苯基-1H-环戊烯并[B]苯并呋喃-2-羧酸甲酯
(1R,2R)-N-[[[6-(2-羧基-2,3-二氢-1H-异吲哚-4-基)-2,2-二甲基己基]氧]羰基]-3-甲基-L-缬氨酰-(4R)-4-羟基-L-脯氨酰-1-氨基-N-(环丙基磺酰基)-2-乙基环丙甲酰胺(1-2)-内酯 Vaniprevir 923590-37-8 C38H55N5O9S
(1R,2R)-N-[[[6-(2-羧基-2,3-二氢-1H-异吲哚-4-基)-2,2-二甲基己基]氧]羰基]-3-甲基-L-缬氨酰-(4R)-4-羟基-L-脯氨酰-1-氨基-N-(环丙基磺酰基)-2-乙基环丙甲酰胺(1-2)-内酯
(1AR,5S,8S,10R,22aR)-5-(1,1-二甲基乙基)-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-十四氢-14-甲氧基-3,6-二氧代-8H-7,10-亚甲基环丙烷并[18,19][1,10,3,6]二氧杂二环草壬基十八碳-7-烯[11,12-b]喹喔啉-8-羧酸 (1aR,5S,8S,10R,22aR)-5-tert-butyl-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradeca-hydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxylic acid hydrate 1206524-85-7 C29H38N4O7
(1AR,5S,8S,10R,22aR)-5-(1,1-二甲基乙基)-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-十四氢-14-甲氧基-3,6-二氧代-8H-7,10-亚甲基环丙烷并[18,19][1,10,3,6]二氧杂二环草壬基十八碳-7-烯[11,12-b]喹喔啉-8-羧酸
(1ALPHA,3BETA,5Z,7E,22E)-24-环丙基-1,3-二羟基-9,10-开环胆甾-5,7,10(19),22-四烯-24-酮 MC903 126860-83-1 C27H38O3
(1ALPHA,3BETA,5Z,7E,22E)-24-环丙基-1,3-二羟基-9,10-开环胆甾-5,7,10(19),22-四烯-24-酮
(11AS,11A'S)-8,8'-(丙烷-1,3-二基双(氧))双(7-甲氧基-2-亚甲基-2,3-二氢-1H-苯并[E]吡咯[1,2-A][1,4]二氮杂卓-5(11AH)-酮) 1,1'-[[(propane-1,3-diyl)dioxy]bis[(11aS)-7-methoxy-2-methylidene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one]] 232931-57-6 C31H32N4O6
(11AS,11A'S)-8,8'-(丙烷-1,3-二基双(氧))双(7-甲氧基-2-亚甲基-2,3-二氢-1H-苯并[E]吡咯[1,2-A][1,4]二氮杂卓-5(11AH)-酮)
(+/-)-6-氯-7,8-二羟基-3-烯丙基-1-苯基-2,3,4,5-四氢-1H-3-苯氮杂卓氢溴酸 SKF 82958 80751-65-1 C19H20ClNO2
(+/-)-6-氯-7,8-二羟基-3-烯丙基-1-苯基-2,3,4,5-四氢-1H-3-苯氮杂卓氢溴酸
(+)-丁苯那嗪 tetrabenazine 1026016-83-0 C19H27NO3
(+)-丁苯那嗪
(+)-JQ1羧酸 (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetic acid 202592-23-2 C19H17ClN4O2S
(+)-JQ1羧酸
—— N-cyclohexyl-3-(3,4-dichlorophenethylamino)-N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethylamino)ethyl)propanamide bis(trifluoroacetate) 1035227-44-1 2C2HF3O2*C29H38Cl2N4O4
N-cyclohexyl-3-(3,4-dichlorophenethylamino)-N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethylamino)ethyl)propanamide bis(trifluoroacetate)
—— Guadecitabine 929901-49-5 C18H24N9O10P
Guadecitabine
—— 1356922-29-6 C18H24N2NaO5
—— (2E)-4,4,4-trifluoro-2-[(3-methylphenyl)hydrazinylidene]-1-thiophen-2-ylbutane-1,3-dione 263890-70-6 C15H11F3N2O2S
(2E)-4,4,4-trifluoro-2-[(3-methylphenyl)hydrazinylidene]-1-thiophen-2-ylbutane-1,3-dione
—— 4-[(2S,7R)-10,11-dimethyl-8-methylidene-1,5,11-triazatricyclo[7.4.0.02,7]tridec-9-en-5-yl]-1-(4-fluorophenyl)butan-1-one 313368-91-1 C23H30FN3O
4-[(2S,7R)-10,11-dimethyl-8-methylidene-1,5,11-triazatricyclo[7.4.0.02,7]tridec-9-en-5-yl]-1-(4-fluorophenyl)butan-1-one
—— (R)-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide 848193-69-1 C13H13ClN2O
(R)-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
—— N-[2-[(2Z)-2-[1-(3-bromophenyl)ethylidene]hydrazinyl]-2-oxo-1-(4-oxo-3H-phthalazin-1-yl)ethyl]benzamide 916170-19-9 C25H20BrN5O3
N-[2-[(2Z)-2-[1-(3-bromophenyl)ethylidene]hydrazinyl]-2-oxo-1-(4-oxo-3H-phthalazin-1-yl)ethyl]benzamide
—— sodium salt of 1-(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)-3-[4-(1-hydroxy-1-methyl-ethyl)-furan-2-sulfonyl]-urea 256373-96-3 C20H23N2O5S*Na
sodium salt of 1-(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)-3-[4-(1-hydroxy-1-methyl-ethyl)-furan-2-sulfonyl]-urea
—— (2S)-2-deuterio-2-(trideuteriomethyl)spiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrochloride 107220-28-0 C10H18ClNOS
(2S)-2-deuterio-2-(trideuteriomethyl)spiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrochloride
—— (H-Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-[Statine(3S,4S)]-Val-Ala-Glu-Phe-OH) 350228-37-4 C73H118N16O27
(H-Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-[Statine(3S,4S)]-Val-Ala-Glu-Phe-OH)
—— Norpseudotropanol 501-33-7 C7H13NO
Norpseudotropanol
—— Tetralithium-4-thiouridin-5'-triphophat 20188-72-1 C9H11N2O14P3S*4Li
Tetralithium-4-thiouridin-5'-triphophat
—— Huhs015 1453097-13-6 C19H18N4O
Huhs015
—— (3S,5R)-6‘-bromo-4-methoxy-3,5-dimethyl-spiro [cyclohexane-1,2’-indane]-1‘-one 1454700-89-0 C17H21BrO2
(3S,5R)-6‘-bromo-4-methoxy-3,5-dimethyl-spiro [cyclohexane-1,2’-indane]-1‘-one
—— S-2765,Chromogenic Substrate for Fxa 115388-96-0 C27H36N8O5
S-2765,Chromogenic Substrate for Fxa
—— K145 hydrochloride 1449240-68-9 C18H24N2O3S*ClH
K145 hydrochloride
—— 96293-19-5 C27H25N3NiO3*(x)H2O
—— KH-CB19 1354037-26-5 C15H13Cl2N3O2
KH-CB19
—— Spirostan-6-one, 3-hydroxy-, (5a,25R)- 1177-71-5 C27H42O4
Spirostan-6-one, 3-hydroxy-, (5a,25R)-
—— Zacopride fumarate 101303-98-4 C4H4O4*C15H20ClN3O2
Zacopride fumarate
—— (5E)-7-{6-[(1E)-3-Hydroxy-1-octen-1-yl]-2-oxabicyclo[2.2.1]hept-5-yl}-5-heptenoic acid 56985-40-1 C21H34O4
(5E)-7-{6-[(1E)-3-Hydroxy-1-octen-1-yl]-2-oxabicyclo[2.2.1]hept-5-yl}-5-heptenoic acid
—— Thymidine-5'-triphosphate, sodium(1:X) 18423-43-3 C10H17N2Na3O14P3
Thymidine-5'-triphosphate, sodium(1:X)
—— tenofovir alafenamide fumarate 379270-38-9 0C4H4O4*C21H29N6O5P
tenofovir alafenamide fumarate
—— BIX02565 1311367-27-7 C26H30N6O2
BIX02565
—— (4E)-4-[[3-[(3-methylphenyl)methoxy]phenyl]methylidene]-1-phenylpyrazolidine-3,5-dione 429653-73-6 C24H20N2O3
(4E)-4-[[3-[(3-methylphenyl)methoxy]phenyl]methylidene]-1-phenylpyrazolidine-3,5-dione
—— (6R oder S)-5,6,7,8-Tetrahydro-Lbioterin-dihydrochlorid 69056-38-8 C9H15N5O3*2ClH
(6R oder S)-5,6,7,8-Tetrahydro-Lbioterin-dihydrochlorid
—— 12-sulfodehydroabietic acid disodium salt 86408-71-1 C20H26O5S*2Na
12-sulfodehydroabietic acid disodium salt
—— Bio-32546 1548743-66-3 C28H31F6NO3
Bio-32546
—— (1R,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-5,6-dihydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol 50648-94-7 C27H44O4
(1R,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-5,6-dihydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
—— mono-L-aspartyl chlorin e6 tetrasodium salt 220201-34-3 C38H37N5O9*4Na
mono-L-aspartyl chlorin e6 tetrasodium salt
—— 17α-hydroxydigitoxigenin 26629-41-4 C23H34O5
17α-hydroxydigitoxigenin
—— (3R,5Z,7E,24S)-9,10-Secocholesta-5,7,10-triene-3,24,25-triol 40013-87-4 C27H44O3
(3R,5Z,7E,24S)-9,10-Secocholesta-5,7,10-triene-3,24,25-triol
—— eldecalcitol 104121-92-8 C30H50O5
eldecalcitol
—— AGN 194310 229961-45-9 C28H24O2S
AGN 194310