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Ready-to-use Cell Proliferation Reagent, WST-1 In conclusio
2022-06-17

In conclusion, the present study demonstrated that peripheral nerve exposure to HIV gp120 increased the expression levels of the P2Y12 receptor in DRG SGCs and enhanced mechanical and thermal hyperalgesia in rat models. Up-regulation of the P2Y12 receptor in DRG SGCs further promoted the release of
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Overall ABC transporters are hypothesised to prevent
2022-06-17

Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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In addition to the increase of extracellular glutamate ICH c
2022-06-17

In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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br Introduction L Glutamate is
2022-06-17

Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of azacytidine functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At elevated concent
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pituitary adenylate cyclase-activating peptide Several studi
2022-06-17

Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upregu
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Clinical trials of all GSIs have ended
2022-06-17

Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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br Introduction The mammalian skin forms
2022-06-17

Introduction The mammalian skin forms the largest organ of the body and includes a network of cutaneous nerves, cells of the immune system, and mediators of the neuro-endocrine axis (Theoharides et al., 2016). Analogous to the hypothalamic-pituitary-adrenal axis, neuropeptides and their receptors
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The activation of GPR FFA signaling
2022-06-17

The activation of GPR40/FFA1 signaling triggers the PLC/PIP2 signaling pathway and results in Ca2+ release from the endoplasmic reticulum (ER). Increased Ca2+ levels may lead to activation of different protein kinases, such as Ca2+/calmodulin-dependent protein kinase type IV, Akt, extracellular sign
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Free fatty acids FFAs which are obtained from
2022-06-17

Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty 2-Chlorotrityl Chloride Resin mg receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors
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The Ala to Leu substitution would reduce the
2022-06-17

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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Combination inhibitors of FAAH TRPV and or COX may
2022-06-17

Combination inhibitors of FAAH, TRPV1, and/or COX2 may have the advantage of effective pain relief with a high therapeutic index. For example, arachidonoyl serotonin (AA-5-HT) inhibits both FAAH (IC=1–12μM) and TRPV1 (IC=37–270nM against 100nM capsaicin in HEK-293 cells)., In mice, AA-5-HT had grea
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Several mechanisms have been suggested to
2022-06-16

Several mechanisms have been suggested to underline the release of signalling molecules from astrocytes: reverse operation of glutamate transporters, volume-regulated anion channels, gap-junctional hemi channels, diffusional release through purinergic receptors and Ca2+-dependent exocytosis [2], [15
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One important aspect about GSK
2022-06-16

One important aspect about GSK-3 inhibitors is their effect on pluripotency of CD 2665 [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combination of events preserv
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Eeyarestatin I While the specific set of
2022-06-16

While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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Targeting MCTs is likely to have dramatic effects on lactate
2022-06-16

Targeting MCTs is likely to have dramatic effects on lactate-dependent metabolic symbiosis described in the previous paragraphs. A plethora of MCT inhibitors have been described, including α-cyano-4-hydroxycinnamate (CHC) [59], organomercurials [60], stilbene disulfonates [60], and other second-gene
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