“leukotriene receptor”的搜索结果
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5-HT Receptor 激动剂
Prucalopride是一种选择性的,高亲和力的5-HT4受体激动剂,作用于5-HT4A和5-HT4B受体,Ki分别为2.5 nM和8 nM,比作用于5-HT受体亚型选择性高290倍以上。
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- Pierre Meschin, .et al. p11 modulates calcium handling through 5-HT4R pathway in rat ventricular cardiomyocytes., Cell Calcium, 2015, Dec;58(6):549-57 PMID: 26427584
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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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Histamine Receptor antagonis
Clemastine fumarate是一种选择性的组胺H1拮抗剂。它与组胺H1受体结合,从而阻断了内源性组胺的作用,从而暂时缓解了由组胺引起的阴性症状。
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α1-adrenergic receptor 激动剂
Phenylephrine HCl是一种选择性的α1肾上腺素能受体激动剂,主要用作减充血剂,扩张瞳孔和增加血压的药物。
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β1 adrenergic receptor blocker
Bisoprolol fumarate是一种属于β受体阻滞剂的药物,β受体阻滞剂是一类主要用于心血管疾病的药物。更具体地说,它是一种选择性的β1肾上腺素能受体阻滞剂。
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Glucocorticoid Receptor 激动剂
Betamethasone Dipropionate是糖皮质激素类固醇,具有抗炎和免疫抑制特性。
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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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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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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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muscarinic receptor 拮抗剂
Tolterodine tartrate (Detrol LA)是毒蕈碱受体拮抗剂。
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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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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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Dopamine Receptor 激动剂
Rotigotine hydrochloride是一种多巴胺D2和D3受体激动剂。D2和D3的Ki值分别为13和0.71 nM。
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- Mattia Ferraiolo, .et al. Dopamine D2L receptor density influences the recruitment of β-arrestin2 and Gi1 induced by antiparkinsonian drugs, Neuropharmacology, 2022, 207: 108942
- Mattia Ferraiolo, .et al. Receptor density influences ligand-induced dopamine D 2L receptor homodimerization, Eur J Pharmacol, 2021, Nov 15;911:174557 PMID: 34626593
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MT1/MT2-Receptor 激动剂
Ramelteon (TAK-375)是melatonin受体激动剂,对褪黑激素MT1(IC50 = 28.5±8.55 pM)和MT2(20.1±9.25 pM)受体均具有高亲和力,并且相对于MT3受体具有选择性。
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Nicotinic (α7) Receptor Modulator
PNU-120596是α7神经元烟碱型乙酰胆碱受体的正变构调节剂。
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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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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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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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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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NOP receptor 激动剂
MCOPPB 3HCl是一种用作伤害感受器受体的有效和选择性激动剂的化合物,pKi为10.07。
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Retinoid X Receptor Ligand
Bexarotene (LGD1069)是一种高度选择性的类维生素A X受体(RXR)激动剂。
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Opioid Receptor 激动剂
ADL5859 HCl是高效的选择性δ阿片受体激动剂,Ki值为0.84 nM,ED50值为20 nM。
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Androgen Receptor 激动剂
Andarine (GTX-007)是研究性的选择性雄激素受体调节剂(SARM)。
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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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Estrogen/progestogen Receptor 激动剂
Hexestrol是一种致癌的合成雌激素,可抑制微管聚合和带状结构的形成。它是脂质过氧化的抑制剂。
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Adrenergic Receptor 激动剂
Salbutamol sulfate (Albuterol)是一种短效β2肾上腺素能受体激动剂。
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Adrenergic Receptor 激动剂
Synephrine (Oxedrine)是一种通常用于减肥的胺化合物。
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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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5-HT4-receptor 激动剂
Mosapride citrate起5-HT4受体激动剂和5-HT3受体拮抗剂的作用。
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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 Modulators
Ostarine (MK-2866,GTX-024)是一种雄激素受体调节剂(SARM)。
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