“…Also worth examining are BMP antagonists, major regulators of these proteins. Evidence has shown that BMPs (especially BMP4/6/7) and BMP antagonists (especially Gremlin1 and follistatin-like protein 1) play essential roles in IBD pathogenesis. …”
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“…The S009 is a known CCR4 antagonist. Now, a series of new thiourea derivatives have been synthesized. …”
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“…In the present work, 9,11-seco-cholesterol derivatives were designed and synthesized by cleaving the C ring of cholesterol and were identified as novel structures of FXR antagonists. Compound 9a displayed the best FXR antagonistic activity at the cellular level (IC(50) = 4.6 μM) and decreased the expression of the target genes of FXR in vivo.…”
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“…Compound 1, which we have previously reported as a potent antagonist of CCR4, was employed as the positive control. …”
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“…We also determined whether these novel CCR4 antagonists could alleviate allergic asthma in a mouse. …”
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“…A series of pyrido[2,3-d]pyrimidine derivatives were designed and synthesized based on known CC chemokine receptor 4 (CCR4) antagonists. The activities of all the newly synthesized compounds were evaluated using a chemotaxis inhibition assay. …”
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“…Using a double-blind, randomised, sham- and placebo-controlled design, this study investigated the influence of DRD2 antagonist on rTMS-induced analgesia and corticospinal excitability across the M1 and DLPFC. …”
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“…In addition, RNA-seq analysis of purified gonadotropes from control and cKO males revealed a profound decrease in expression of gremlin (Grem1), a bone morphogenetic protein (BMP) antagonist. We show Grem1 was expressed in gonadotropes, but not other cell lineages, in the adult male mouse pituitary. …”
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“…BACKGROUND: There is limited literature investigating the effects of body mass index (BMI) and androgen level on in vitro fertilization (IVF) outcomes with a gonadotropin-releasing hormone (GnRH)-antagonist protocol in polycystic ovary syndrome (PCOS). …”
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“…CIRBP-mediated cytoprotection against doxorubicin-induced cardiac apoptosis was demonstrated to largely involve OGFR repression by CIRBP. NTX as a potent antagonist of OGFR successfully rescued CIRBP ablation-rendered susceptibility to cardiac dyshomeostasis upon exposure to doxorubicin, whereas another antagonist ALV acting only on opioid receptors did not. …”
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“…The alpha 2-adrenoceptor (α(2)-AR) antagonist yohimbine and α(2A)-ARs antagonist BRL-44408 maleate were systemically administered to rats to determine the effects of α(2A)-ARs on NE release in the PVN. …”
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“…We also found that pre-treatment with the purinergic P2R antagonist suramin inhibits HRV-enhanced MUC5AC expression and protein release, implicating involvement of purinergic signaling by extracellular ATP. …”
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“…In subgroup analysis, GH treatment significantly increased the day 3 embryos available rate in the subgroup of young PORs with the long down-regulation (63.11 vs. 49.35%; p = 0.004), while significantly reduced the risk of miscarriage in the subgroup of young PORs with GnRH antagonist protocol (0.00 vs. 12. %; p = 0.023). There was no significant difference for LBR in PORs with GnRH antagonist (<35 years [35.19 vs. 28.45%; p = 0.183]; ≥35 years [12.96 vs. 14.03%; p = 0.707]), GnRH-a long (<35 years [33.33 vs. 36.99%; p = 0.597]; ≥35 years [17.44 vs. 20.28%; p = 0.574]) and long down-regulation (<35 years [58.82 vs. 41.90%; p = 0.193]; ≥35 years [43.33 vs. 25.30%; p = 0.065]). …”
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“…Accordingly, a specific antagonist of the Htr1a receptor decreases food intake in leptin-deficient but not in Htr1a(−/−) mice. …”
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“…Ketamine, an N-methyl-D-aspartate receptor antagonist, is widely used as a general pediatric anesthetic. …”
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“…In addition, the present findings suggested that Rg1 was a potent PPARγ agonist in that it upregulated PPARγ expression and was inhibited by GW9662, a selective PPARγ antagonist. These findings expand our previous understanding of the molecular basis of the therapeutic action of Rg1 in cerebral ischemic injury, laying the ground work for expanded study and clinical optimization of the compound.…”
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“…Western blotting was used to determine protein levels of the apoptosis-associated regulators, cleaved caspase 3, B-cell lymphoma-2 (Bcl-2)-associated X protein (Bax), Bcl-2 homologous antagonist/killer (Bak) and Bcl-extra large (Bcl-xl), as well as the cell cycle-related regulators, p21 and p27. …”
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“…In MPTP parkinsonian mice, micro-pressure application of the selective HCN channel antagonist, ZD7288, decreased the firing rate in 10 out of the 28 pallidal neurons, while increased the firing rate in another 15 out of the 28 neurons. …”
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“…E. coli RNA-stimulated transforming growth factor beta 1 (TGF-β1) overproduction in HSC-T6 cells, which was blocked by recombinant IL-1 receptor antagonist (rIL-1Ra) or nuclear factor κB inhibitor BAY 11-7082. …”
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