“leukotriene receptor”的搜索结果
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S1P Receptor 拮抗剂
FTY720 (Fingolimod)是ISP-1(肉豆蔻酸)的衍生物，ISP-1是中国草药Iscaria sinclarii的真菌代谢物，也是鞘氨醇的结构类似物。
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- Tina Sepasi, .et al. Targeted gene delivery to the brain using CDX-modified chitosan nanoparticles, BioImpacts, 2022, 28 May
- Zengzi Zhou, .et al. Effects of immunomodulatory drug Fingolimod (FTY720) on Chlamydia dissemination and pathogenesis, Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. Inulooligosaccharides in Atractylodis lanceae rhizoma and Atractylodis rhizoma of hochuekkito formula are essential for regulation of the pulmonary immune system of immuno-compromised mice, Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. 14-3-3 signal adaptor and scaffold proteins mediate GPCR trafficking, Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. Peyer's patch-immunomodulating glucans from sugar cane enhance protective immunity through stimulation of the hemopoietic system, Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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Androgen Receptor 拮抗剂
Bicalutamide (Casodex)是一种口服非甾体抗雄激素，用于治疗前列腺癌和多毛症。
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- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells, Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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LPA Receptor 拮抗剂
ki16425是对LPA1和LPA3具有选择性的LPA受体拮抗剂，对人LPA1、LPA2和LPA3受体分别显示Ki值为0.34、6.5和0.93 μM。
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- Maria F Fernandes, .et al. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid, Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. Lateral access mechanism of LPA receptor probed by molecular dynamics simulation, PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. Illuminating G-Protein-Coupling Selectivity of GPCRs, Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA6, Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. Generalized pruritus in primary sclerosing cholangitis: implications of histamine release by lysophosphatidic acid., Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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Androgen Receptor 拮抗剂
Cyproterone acetate是17-羟孕酮的合成衍生物，可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。
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neurokinin-1 receptor 拮抗剂
Aprepitant (MK-0869)被归类为NK1拮抗剂。已经显示，阿瑞匹坦通过阻止P物质降落在大脑神经元受体上，从而抑制细胞毒性化疗药物引起的急性呕吐和延迟呕吐。还显示出它能增加5-HT3受体拮抗剂恩丹西酮和皮质类固醇地塞米松的活性，它们也可用于预防化学疗法引起的恶心和呕吐。
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- Kodji X, .et al. Sensory nerves mediate spontaneous behaviors in addition to inflammation in a murine model of psoriasis, FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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5-HT2B receptor 拮抗剂
RS-127445是5-羟色胺5-HT2B受体的有效和选择性拮抗剂，相对于密切相关的5-HT2A和5-HT2C受体具有约1000倍的选择性。
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- Takeshi Takayanagi, .et al. Serotonin 5-HT2B receptor antagonism is fundamental for protecting PC12 cells exposed to hydrogen peroxide, Fujita Medical Journal, 2015, 1(1), 1-5, 2015
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muscarinic receptor 拮抗剂
5-hydroxymethyl tolterodine (PNU 200577)是托特罗定的代谢产物，tolterodine是一种用于治疗尿失禁的毒蕈碱受体拮抗剂。
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AT1 receptor 拮抗剂
Eprosartan是一种用于治疗高血压的血管紧张素II受体拮抗剂。
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Muscarinic receptor antagonist
Biperiden HCl是毒蕈碱受体拮抗剂，对M1亚型表现出一定的选择性。
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muscarinic receptor 拮抗剂
Tolterodine tartrate (Detrol LA)是毒蕈碱受体拮抗剂。
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muscarinic M3 receptor antagoinst
Solifenacin succinate是毒蕈碱M3受体拮抗剂，用于治疗尿失禁。
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EndothelinA receptor 拮抗剂
Ambrisentan (BSF 208075)充当内皮素受体拮抗剂，对A型内皮素受体（ETA）具有选择性。
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- Naoki Dohi, .et al. Quantitative real-time measurement of endothelin-1-induced contraction in single non-activated hepatic stellate cells, PLoS One, 2021, 16(8): e0255656 PMID: 34343209
- Tony Ngo, .et al. Orphan receptor ligand discovery by pickpocketing pharmacological neighbors, Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
- Toshiaki Okamoto, .et al. Antifibrotic effects of ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model, World J Hepatol, 2016, Aug 8; 8(22): 933-941 PMID: 27574547
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Opioid 拮抗剂
Alvimopan (ADL 8-2698)表现为外周作用的opioid拮抗剂，Alvimopan竞争性结合胃肠道中的mu-opioid receptor。
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A2a receptor 拮抗剂
SYN115是口服，有效和选择性的腺苷2a（A2a）受体抑制剂，作用于人类和恒河猴的 adenosine A2A 受体，Ki 值分别为 11.5 nM 和 6 nM。
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P2X7 receptor 拮抗剂
A740003是P2X7受体的新型竞争性拮抗剂（人的IC50值= 40 nM，大鼠的IC50值= 18 nM）。
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Estrogen receptor 拮抗剂
Tamoxifen Citrate是哺乳动物甾醇异构酶的选择性和有效抑制剂。
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- Renu Sudhakar, .et al. Bazedoxifene, a Postmenopausal Drug, Acts as an Antimalarial and Inhibits Hemozoin Formation, Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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P2Y6 Receptor 拮抗剂
MRS 2578是P2Y6核苷酸受体的选择性拮抗剂。
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5-HT7 receptor 拮抗剂
SB269970 HCl是有效的选择性5-HT7受体拮抗剂。
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NMDA receptor 拮抗剂
Memantine hydrochloride是nmda受体的拮抗剂，与离子通道位点结合。它还是CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，Ki分别为0.51 nM和94.9 μM。它被用于治疗帕金森综合征。
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NMDA receptor 拮抗剂
Orphenadrine柠檬酸盐是NMDA受体拮抗剂，Ki为6.0μM，还是HERG钾离子通道阻断剂。
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NMDA Receptor 拮抗剂
TCN 201是对NR1/NR2A相对于含NR1/NR2B的受体具有选择性的NMDA受体拮抗剂。
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Adenosine receptor 拮抗剂
Aminophylline是一种非选择性的腺苷受体拮抗剂和磷酸二酯酶抑制剂，能够逆转局部缺血引起的bradyasystole。
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Adenosine receptor 拮抗剂
Dyphylline是黄嘌呤衍生物，具有支气管扩张药和血管扩张药的作用。 它充当腺苷受体拮抗剂和磷酸二酯酶抑制剂。
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5-HT2A serotonin receptor 拮抗剂
Ketanserin (Vulketan Gel)是大鼠和人5-HT2A血清素受体拮抗剂，Ki为2.5 nM。
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neurokinin-1 receptor 拮抗剂
MK-0517 (Fosaprepitant,L-758,298)是Aprepitant的水溶性磷酰基前药，它是NK1拮抗剂。
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5-HT3 receptor 拮抗剂
Granisetron Hydrochloride是血清素5-ht3受体拮抗剂。
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OX receptor 拮抗剂
Suvorexant (MK-4305)是OX1R和OX2R的有效，选择性和口服可生物利用的拮抗剂，目前正在临床研究中作为失眠的新疗法。
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- Richard L Spinieli, .et al. Orexin contributes to eupnea within a critical period of postnatal development, Am J Physiol Regul Integr Comp Physiol, 2021, Oct 1;321(4):R558-R571 PMID: 34405704
- Jacob W Clark, .et al. Manipulation of REM sleep via orexin and GABAA receptor modulators differentially affects fear extinction in mice: effect of stable versus disrupted circadian rhythm, Sleep, 2021, Mar 15;zsab068 PMID: 33720375
- Zhang B, .et al. Hypothalamic orexin and mechanistic target of rapamycin activation mediate sleep dysfunction in a mouse model of tuberous sclerosis complex, Neurobiol Dis, 2019, Oct 9;134:104615 PMID: 31605778
- Obara K, .et al. Assessment of Inhibitory Effects of Hypnotics on Acetylcholine-Induced Contractions in Isolated Rat Urinary Bladder Smooth Muscle, Biol Pharm Bull, 2019, 42(2):280-288 PMID: 30713259
- James B Jaggard, .et al. Hypocretin underlies the evolution of sleep loss in the Mexican cavefish, eLife, 2018, 7: e32637 PMID: 29405117
- Skillman B, .et al. Quantification of suvorexant in blood using liquid chromatography-quadrupole/time of flight (LC-Q/TOF) mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2018, Aug 1;1091:87-95 PMID: 29859493
- Clark L, .et al. On the use of Pichia pastoris for isotopic labeling of human GPCRs for NMR studies, J Biomol NMR, 2018, Aug;71(4):203-211 PMID: 30121871
- Sullinger S, .et al. Identification of Suvorexant in Urine Using Liquid Chromatography-Quadrupole/Time-of-Flight Mass Spectrometry (LC-Q/TOF-MS), J Anal Toxicol, 2017, Apr 1;41(3):224-229 PMID: 28035034
- Carson M, .et al. Quantification of suvorexant in urine using gas chromatography/mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2017, Jan 1;1040:289-294 PMID: 27825624
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ETA receptor 拮抗剂
Sitaxsentan sodium (TBC-11251)是一种选择性内皮素受体A拮抗剂，IC50和Ki分别为1.4 nM和0.43 nM。
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vasopressin receptor 2 拮抗剂
Tolvaptan是一种选择性的竞争性精氨酸加压素受体2拮抗剂，IC50为1.28μM。
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OX Receptor 拮抗剂
SB-408124是一种选择性的非肽orexin OX1受体拮抗剂(人OX1和OX2受体的Kb值分别为21.7和1405 nM)。体内口服后阻断orexin-A诱导的修饰。
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somatostatin receptor 拮抗剂
Octreotide是sst2，sst3和sst5生长抑素受体的肽激动剂。克隆的人类生长抑素受体的IC50/Kd值（nM）为：290-1140（sst1），0.4-2.1（sst2），4.4-34.5（sst3），> 1000（sst4）和5.6-32（sst5）。
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OX1 receptor 拮抗剂
SB 334867是一种选择性的非肽orexin OX1受体拮抗剂。对于分别表达人OX1和OX2受体的CHO细胞中的细胞内Ca2 +释放抑制，pKb值为7.2和<5。体内全身给药后，阻断orexin-A诱导的美容和进食。
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- Tony Ngo, .et al. Orphan receptor ligand discovery by pickpocketing pharmacological neighbors, Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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5-HT Receptors/D2 dopamine receptor 拮抗剂
Olanzapine (LY170053)对5-HT2血清素和D2多巴胺受体拮抗剂具有高亲和力。
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Dopamine Receptor 拮抗剂
Paliperidone (Invega)是一种非典型的抗精神病药。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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angiotensin AT2 receptor 拮抗剂
PD 123319 ditrifluoroacetate是一种有效的，选择性的非肽血管紧张素AT2受体拮抗剂。大鼠肾上腺组织和大脑的IC50值分别为34和210 nM。
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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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β2 adrenergic 拮抗剂
ICI 118,551 hydrochloride是选择性的β2 adrenergic receptor 拮抗剂,结合 β2，β1 和 β3 肾上腺素能受体的Ki 值分别为 0.7，49.5 和 611 nM。
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AMPA Receptor 拮抗剂
NBQX是一种有效，选择性和竞争性的AMPA受体拮抗剂。
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NMDA receptor 拮抗剂
MDL-29951是在体外和体内均能激活NMDA受体的新型甘氨酸拮抗剂（Ki = 0.14 mM，[3H]甘氨酸结合）。
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Dual orexin receptor 拮抗剂
TCS 1102是一种有效的双重食欲素受体拮抗剂（OX2和OX1受体的Ki值分别为0.2和3 nM）。
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5-HT2C serotonin receptor 拮抗剂
N-Desmethylclozapine是一种有效的选择性5-HT2C血清素受体拮抗剂。
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Dopamine receptor 拮抗剂
cis-(Z)-Flupentixol dihydrochloride是多巴胺受体拮抗剂、抗精神病药物、抗精神病药物。
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sigma-1 receptor 拮抗剂
S1RA是一种选择性sigma-1受体拮抗剂，据报道其结合亲和力为Ki = 17.0±7.0 nM，对sigma-2受体具有选择性，并且对其他170种受体，酶，转运蛋白和离子通道具有选择性。
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CB1 receptor 拮抗剂
AM251是有效的CB1受体拮抗剂（IC50 = 8 nM，Ki = 7.49 nM），其选择性是CB2受体的306倍。
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5-HT Receptor 拮抗剂
Tandospirone是5HT1A受体的部分激动剂。它以剂量依赖性方式显着降低氟哌啶醇诱导的运动迟缓。
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CRTH2 receptor 拮抗剂
AZD1981作为疾病相关细胞系统的有效拮抗剂，可抑制DK-PGD2诱导的人嗜酸性粒细胞CD11b表达，IC50为10 nM。
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Angiotensin II receptor 拮抗剂
Tasosartan是一种血管紧张素II受体拮抗剂。
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NK1 receptor 拮抗剂
Rolapitant，也称为SCH-619734，是一种选择性的，可生物利用的CNS渗透性神经激肽NK1受体拮抗剂，在呕吐动物模型中显示出行为效应。
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- Bubak AN, .et al. Varicella Zoster Virus Induces Nuclear Translocation of the Neurokinin-1 Receptor, Promoting Lamellipodia Formation and Viral Spread in Spinal Astrocytes, J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
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5-HT6 receptor 拮抗剂
SB-742457是一种选择性的5-HT6受体拮抗剂，具有认知，记忆和增强学习的作用。
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LPA1 receptor 拮抗剂
AM966是LPA1受体（溶血磷脂酸受体）的高亲和力，选择性口服拮抗剂，IC50值为17 nM。
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- Maria F Fernandes, .et al. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid, Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
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neuropeptide Y Y2 receptor 拮抗剂
JNJ-31020028是一种新型的选择性脑渗透神经肽Y Y2受体拮抗剂。
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