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We next turned our attention to the
2021-08-27

We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional a
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Central to the mechanism of cold
2021-08-26

Central to the mechanism of cold I/R-associated liver injury is the activation of the pro-inflammatory cascade resulting in the release of pro-inflammatory cytokines. In agreement with the present study, serum and hepatic mRNA levels of TNF-α, IL-6, and ICAM-1 were all significantly up-regulated ear
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Twin studies have shown that P
2021-08-26

Twin studies have shown that P has moderate heritability. Zuckerman (1989) reviewed the earlier studies of P or related traits and found a median heritability of 0.51. However, twin studies using an Eysenckian P scale have tended to estimate somewhat lower heritabilities than this, in the range 0.36
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Introduction Amphetamine AMPH methamphetamine MA and
2021-08-26

Introduction Amphetamine (AMPH), methamphetamine (MA), and 3,4-ethylenedioxymethamphetamine (MDMA) are widely abused psychoactive substances, with the basic chemical structure of phenylethylamine [1]. The abuse of these drugs is associated with psychostimulant, anorectic and hallucinogenic properti
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Several research groups have disclosed potent and
2021-08-26

Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2
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Our data show a site
2021-08-26

Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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Widely expressed mammalian adhesion receptors for fibrillar
2021-08-26

Widely expressed mammalian adhesion receptors for fibrillar collagens include the α2β1- and α11β1-integrins and the discoidin domain receptors (DDRs), DDR1 and DDR2 (Leitinger, 2011). Integrins and DDRs bind distinct and separate motifs in native fibrillar collagen (Curat et al., 2001, Vogel et al.,
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Our recent discovery M P H
2021-08-26

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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br Materials and methods br Results br Discussion CHIKV is
2021-08-26

Materials and methods Results Discussion CHIKV is an important arthropod borne virus with substantial impact on global health and cause a major viral disease that requires the development of antiviral drug to combat chikungunya disease. Virus specific proteases have particularly become an a
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Some studies have demonstrated that BMSCs can provide severa
2021-08-26

Some studies have demonstrated that BMSCs can provide several trophic and growth factors that play important roles in cell survival, angiogenesis, and BMSC differentiation, but not cell replacement (Peled et al., 1999, Shen et al., 2007, Ji et al., 2004). This paracrine effect of BMSCs is a potentia
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Introduction The first reference to a
2021-08-26

Introduction The first reference to a possible involvement of orexins in the effects of drugs of abuse appeared in 2003 and showed that orexigenic peptide neurons respond to the chronic administration of morphine followed by abrupt withdrawal symptoms caused by opioid receptor antagonists (Georgesc
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The mechanisms in the central nervous system
2021-08-26

The mechanisms in the central nervous system (CNS) controlling the sympathetic tone of the rho kinase inhibitor are associated to behavioral strategies, such as those involved in response to stress. In this regard, morphine withdrawal induces profound and severe stress reactions evidenced by enhanc
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AT13148 It is now known that cholinergic
2021-08-26

It is now known that cholinergic signaling plays a vital role in controlling many peripheral functions including skeletal and smooth muscle contraction, autonomic postganglionic neuron activation, parasympathetic end-organ activation (e.g., salivary, lacrimal and bronchial glands), regulation of car
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br Acknowledgments Denise Fernandes acknowledges a postdoc f
2021-08-26

Acknowledgments Denise Fernandes acknowledges a postdoc fellowship (SFRH/BPD/34289/2006) from the Portuguese Fundação para a Ciência e Tecnologia (FCT) of the Ministry of Science and Technology of Portugal. This work was supported by the Spanish National Plan for Research (Project Ref. CGL2011-24
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Our results showed that in elastase induced AAA TGF
2021-08-25

Our results showed that in elastase-induced AAA, TGF-β neutralization finely tunes macrophage phenotype. Note that several studies have already addressed the role of M1 markers, such as IL-6 and IL-1β, or M2 markers, including IL-10 and TGF-β.4, 9, 10, 11 The expression and the role of ARG1 in AAA h
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