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ANTAGONIST - Springer Nature

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Last Updated: 10 August 2022

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The V_2 receptor antagonist tolvaptan counteracts proliferation and invasivity in human cancer cells

Hyponatremia, the most common electrolyte change in clinical practice, has been linked to a reduced prognosis in cancer patients. Low extracellular sodium, according to in vitro studies, aids cancer cell proliferation and invasion. So far, only a few in vitro reports support a direct role of tolvaptan in fighting cancer progression. Tolvaptan cell lines from various tumor cells [i. e. ] The object of this research was to determine the effect and mechanism of action of the drug tolvaptan. [i. e. ] Methods and findings First, we found that these cell lines express the V_2 receptor. With an IC_50 in the micromolar range, Tolvaptan significantly reduced cell proliferation. Conclusions Overall, these results show that tolvaptan effectively stops tumor formation in vitro. Further research will show whether the V_2 receptor could be a prospective target in anti-cancer programs in the future.

Source link: https://doi.org/10.1007/s40618-022-01807-5


Economical Voltammetric Sensor for Sensitive Rapid Determination of Ondansetron in the Presence of Opioid Antagonist Naltrexone

Moreover, the improved electrode MWCNTs/PVP/CPE demonstrated high selectivity in the voltammetric measurements of ondansetron and co-administrated opioid antagonist drug naltrexone, which showed high separation. Ondansetron and naltrexone, respectively, had a linear relationship with drug concentration in the range of with detection limits ranging from 430 pmolL to 456 pmolLu22121 for ondansetron and naltrexone.

Source link: https://doi.org/10.1007/s12678-022-00739-1


A systematic review and meta-analysis of non-vitamin K antagonist oral anticoagulants vs vitamin K antagonists after transcatheter aortic valve replacement in patients with atrial fibrillation

Patients with aortic valvular disease are increasingly undergoing transcatheter aortic valve replacement. Purpose Transcatheter Aortic valve replacement is now available in patients with aortic valvular disease. Despite this, there is still a paucity of data and established guidelines regarding anticoagulation use in patients with AF. Results A total of 25,199 patients with AF were listed in seven papers, with 9764 patients on non-vitamin K antagonist oral anticoagulants and 15,435 patients on vitamin K antagonists included in a series of studies. There were no apparent differences between patients on NOAC and VKA for all-cause mortality at 2 years, stroke within 30 days, stroke within one year, ischaemic stroke at 1 year, and life-threatening bleeding at 30 days. NOAC's findings reveal NOAC as a potential alternative treatment modality to VKA in post-TAVR patients with AF, but further research is required to establish the full safety and efficacy profile of NOAC.

Source link: https://doi.org/10.1007/s00228-022-03371-6


Dynamics and structural changes of calmodulin upon interaction with the antagonist calmidazolium

CaM antagonists are required for basic studies as well as potential therapeutic applications due to their pleiotropic roles in normal and pathological cell functions. Calmidazolium is a potent small molecule antagonist of CaM and one of the most commonly used CaM inhibitors in cell biology. Conclusions We have evidence that binding of a single molecule of CDZ leads to an open-to-closed conformational reorientation of the two domains of CaM, resulting in a rapid settling of the cellular components involved with a decrease of protein kinetics over a long time span. CaM residues in close contact with CDZ and instrumental in the CaM:CDZ complex's stabilization have been found. Conclusions Our results provide molecular insights into CDZ-induced behavior and structural changes of CaM that result in its inhibition, as well as the rational design of more specific CaM antagonists.

Source link: https://doi.org/10.1186/s12915-022-01381-5


Recombinant LH supplementation improves cumulative live birth rates in the GnRH antagonist protocol: a multicenter retrospective study using a propensity score-matching analysis

However, the benefit of recombinant LH supplementation to recombinant follicle stimulating hormone during controlled ovarian stimulation in the gonadotrophin-releasing hormone therapy regimen is uncertain. Methods This multicenter retrospective cohort study found 899 GnRH antagonist cycles in three reproductive centers and matched them to 2652 r-FSH stimulating cycles using propensity score matching for potential confounders in a 1:3 ratio. Both fresh embryo transfer cycles and frozen embryo transfer cycles resulted in a higher 2-pronuclear embryo rate, usable embryo rate, and live birth rate in both fresh embryo transfer cycles and frozen embryo transfer cycles. R-LH supplementation in the GnRH antagonist cycle was significantly associated with a higher CLBR and live birth rate in fresh and FET cycles, as well as improved embryo quality without raising the OHSS rate and cycle cancellation rate.

Source link: https://doi.org/10.1186/s12958-022-00985-4


Gonadotropin releasing hormone (GnRH) antagonist administration to decrease the risk of ovarian hyperstimulation syndrome in GNRH agonist cycles triggered with human chorionic gonadotropin

Hence, we investigated the use of a GnRH antagonist to reduce the risk of OHSS, due to its ability to reduce VEGF production and function. Methods A retrospective cohort study of 171-IVF patients at risk of developing OHSS following a GnRH agonist cycle with HCG trigger was conducted from 2011 to 2019. Women were pushed to a freeze-all cycle and received either cabergoline 0. 5 mg orally alone for 7 days from the purchase orally and ganirelix, 250 mcg SC for 7 days starting with cabergoline 0. 5 mg orally. More abdominal pain and bloating than group 2 were experienced in group 1 than group 2, and the presence of free fluid was more frequent in group 1 than group 2. The use of GnRH antagonists in the luteal phase may reduce the chance of experiencing moderate and severe OHSS in patients at risk of developing moderate and severe OHSS following a hCG trigger in a GnRH agonist cycle.

Source link: https://doi.org/10.1007/s00404-022-06717-8


Agonist-antagonist muscle strain in the residual limb preserves motor control and perception after amputation

With some undergoing a myoneural interface intervention, some amputees' lower leg amputees were exposed to agonist-antagonist muscle strain and motor control and perception. People who have limb amputation may have trouble with managing mobility and recognition of residual limbs. In fourteen people who had undergone lower limb amputations, we used ultrasound imaging and other techniques to determine muscle endurance and limb appearance. We find that the degree at which the relationship between two muscles is preserved is associated with greater ease of limb mobility following amputation. In this research, relationships between preserved agonist-antagonist muscle strain within the residual leg and preserved motor control and perception capacity are investigated. The release of muscle synergies results in a variety of motor control in biologically intact limbs, according to study. We'll look at the naturalness of phantom joint motor control postamputation based on extracted muscle synergies and activation profiles. Keeping limb sensitivity reserves requires more agonist-antagonist muscle strain preservation in comparison to a biologically intact limb, according to identified studies, preserving limb perception capacity requires more agonist-antagonist muscle strain preservation. Conclusions The results show that agonist-antagonist muscle strain is a common, easily identifiable residual limb structural feature that can help explain variation in amputation results, and agonist-antagonist muscle strain preservation preserving surgical amputation techniques are two ways to achieve more effective and biomimetic sensorimotor control post amputation.

Source link: https://doi.org/10.1038/s43856-022-00162-z


Neutrophil extracellular traps are involved in enhanced contact hypersensitivity response in IL-36 receptor antagonist-deficient mice

Mice, Il36rn u2212/u2212 mice have an elevated contact hypersensitivity response as a result of increased neutrophil recruitment, as shown by earlier studies. In addition, Il3612/u2212 mice develop significant psoriatic skin lesions and increased neutrophil extracellular trap formation, which are not present in Il36rn u2212/u2212 mice. Improved CHS responses, increased infiltration of inflammatory cells, including neutrophils, CD4+ T cells, and CD8+ T cells, NET integration, and increased mRNA expression of cytokines and chemokines, including IL-36, including IL-36 billion3. In addition, the NET formation blockade enhanced the CHS' response, resulting in decreased inflammatory cell infiltration and NET formation, which in turn reduced inflammatory cell infiltration and NET formation. These results show that IL-36Ra deficiency contributes to the CHS response, which is exacerbated by excessive inflammation cell recruitment, NET creation, and cytokine and chemokine manufacturing, as well as the NET formation blockade, which improves the CHS response, as shown by this study. Hence, NET formation may play a significant role in the CHS's response.

Source link: https://doi.org/10.1038/s41598-022-16449-z


Effects of Finerenone, a Novel Nonsteroidal Mineralocorticoid Receptor Antagonist, on Cardiovascular Disease, Chronic Kidney Disease, and Blood Pressure

We summarize pre-clinical and clinical studies focusing on the effects of finerenone on these disease processes in this review. Finerenone's early trials show safety and effectiveness in improving renal and cardiovascular outcomes in patients with CKD. Conclusions: Finerenone's addition to the standard of care for certain CKD patients, particularly those with elevated risk of or pre-existing cardiovascular disease, has been largely supported by the scientific findings. Finerenone's effect in diverse patient populations and different disease states is still needed.

Source link: https://doi.org/10.1007/s11886-022-01750-0

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions