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Toxicity is the main reason for the failure at
2024-05-23
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sel
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Syringin synthesis Consistent with the observation that muta
2024-05-23
Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t
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br Conclusion br Acknowledgments The authors extend their
2024-05-22
Conclusion Acknowledgments The authors extend their appreciation to Kayyali Chair for Pharmaceutical Industry, Department of Pharmaceutics, College of Pharmacy, King Saud University for funding this work through the research project Number (G-2016-2). Introduction L-ornithine is a natural
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br Materials and Methods br Results
2024-05-22
Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer imidazoline in vitro, including Hs578T, MCF-7, and MDA-M
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Most clinically approved antiangiogenic drugs are aimed at b
2024-05-22
Most clinically approved antiangiogenic drugs are aimed at blocking the action of vascular endothelial growth factor, or VEGF, which is accepted to be the most important tumor-derived angiogenic factor, stimulating proliferation and migration of endothelial cells, as well as branching of vessels (Fe
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There are no studies documented the role of RAS in
2024-05-22
There are no studies documented the role of RAS in the differentiation of MSCs into IPCs but there are previous studies indicating that Ang II receptors exhibit opposing actions on MSCs differentiation, into other cell types rather than IPCs. The blockade of AT2R was reported to suppress MSCs differ
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Moreover a multiple regression analysis using the year MMSE
2024-05-22
Moreover, a multiple regression analysis using the 1-year MMSE score as a dependent variable was conducted. The result showed that serum dapagliflozin levels at admission did not affect the MMSE score 1 year later (β = 0.10, p = 0.639). Discussion In this study, serum Aβ42 levels were significa
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The present study determined the effect of DCA on VSMC
2024-05-22
The present study determined the effect of DCA on VSMC calcification in vitro and in atherosclerotic ApoE-/- mice in vivo. We found that 5z sale non-toxic concentrations of DCA, did not affect VSMC viability, induced calcification of VSMC in culture and increased atherosclerotic vascular calcificat
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Our co IP data show that HT A
2024-05-22
Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun
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hydroxydopamine OHDA is a selective catecholaminergic neurot
2024-05-22
6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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Previous work established interactions between CRF and KOR
2024-05-22
Previous work established interactions between CRF and KOR systems in regulating attention (39). The CRF antagonist ANT attenuated, but did not completely reverse, the effects of PACAP (.5 µg) and did not have any effects on its own (Table 2). There were no significant differences in performance amo
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Numerous studies have shown that PUFA incorporation into
2024-05-22
Numerous studies have shown that ω-3 PUFA incorporation into the lipid raft can affect the distribution and function of protein in the lipid raft by altering raft composition [25], [26], [27]. For example, DHA treatment excluded phospholipase D (PLD) from lipid raft toward non-lipid raft, resulting
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The present work has implications for
2024-05-21
The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed
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Derivatives of M that possess
2024-05-21
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these gsk-3 to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrated t
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In conclusion we have designed and synthesized a series of
2024-05-21
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative p
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