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MMP-2 Inhibitor II SCH is a H R receptor antagonist introduc
2022-06-07

SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obes
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Although we showed that RBL H Sc cells took up
2022-06-07

Although we showed that RBL-2H3 Sc98 Phosphatase Inhibitor Cocktail 1 (100X in DMSO) took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter so
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opioid receptor br Prostaglandins meet Hippo The prostagland
2022-06-07

Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic opioid receptor by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects against DSS-induced
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Our results show furthermore that higher concentrations
2022-06-07

Our results show furthermore, that higher concentrations of butyric 97 9 additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GSTP1 expression rema
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Evodiamine br Mutagenesis and Receptor Modeling Studies
2022-06-07

Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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Ning et al showed that
2022-06-07

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Continuing studies of endocannabinoid ligands at GPR reveal
2022-06-07

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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Additionally OsGly I overexpressing transgenic rice plants h
2022-06-06

Additionally, OsGly I-overexpressing transgenic rice plants had higher grain yields than WT (Table 2). Although there were no significant differences in the number of effective panicles per plant, panicle length, grain numbers per panicle, or 1000-grain weight between WT and transgenic plants, the s
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Such responses have led to the idea that
2022-06-06

Such responses have led to the idea that elasmobranchs may be glucose intolerant. However, certain species, such as the North Pacific spiny dogfish (Squalus suckleyi; note that the species used in this study was previously referred to as Squalus acanthias but a study by Ebert et al. (2010) provided
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br Introduction Maintaining blood glucose within an
2022-06-06

Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The p53 inhibitor is especially dependent on an adequate, continuous supply of circulating glucose to
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While CART increased circulating levels of
2022-06-06

While CART increased circulating levels of GIP and GLP-1 in vivo, we were unable to detect any effect of exogenous CART on GIP and GLP-1 mRNA expression or GLP-1 secretion in vitro. There is no ready explanation for this discrepancy. The CART doses used (both in vivo and in vitro) have been shown to
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While ghrelin s role in addictive behaviors has
2022-06-06

While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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The ultimate success of multimodal probe in
2022-06-06

The ultimate success of multimodal probe in the inflammation imaging will be dependent on simplicity in synthesis (combining various modules without protection/deprotection), ease of optimization of pharmacological properties (linker group with tunable PEG moiety), co-registration of macroscopic and
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Formyl peptide receptors FPRs are
2022-06-06

Formyl peptide receptors (FPRs) are a family of surface-expressed, G protein-coupled receptors [7]. The three members, FPR1, FPR2 and FPR3, share significant sequence homology, but have different functional properties [7]. While FPRs are mainly expressed by innate leukocytes, they are also found on
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The synthesis route of strobol C
2022-06-06

The synthesis route of strobol C started from kirenol, which was treated with phosphomolybdic Eribulin mesylate synthesis hydrate in acetone to afford isopropylidenkirenol () as illustrated in . Treatment of with acetic anhydride in a mixture of dry pyridine, gave fully protected intermediate in
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