Metabolically Stable Neurotensin Analogs Exert Potent and Long-Acting Analgesia Without Hypothermia [PDF]
The endogenous tridecapeptide neurotensin (NT) has emerged as an important inhibitory modulator of pain transmission, exerting its analgesic action through the activation of the G protein-coupled receptors, NTS1 and NTS2. Whereas both NT receptors mediate the analgesic effects of NT, NTS1 activation also produces hypotension and hypothermia, which may ...
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Pain relief devoid of opioid side effects following central action of a silylated neurotensin analog [PDF]
Neurotensin (NT) exerts naloxone-insensitive antinociceptive action through its binding to both NTS1 and NTS2 receptors and NT analogs provide stronger pain relief than morphine on a molecular basis. Here, we examined the analgesic/adverse effect profile of a new NT(8-13) derivative denoted JMV2009, in which the Pro10 residue was substituted by a ...
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Hydrothermal liquefaction of sewage sludge; energy considerations and fate of micropollutants during pilot scale processing [PDF]
The beneficial use of sewage sludge for valorization of carbon and nutrients is of increasing interest while micropollutants in sludge are of concern to the environment and human health. This study investigates the hydrothermal liquefaction (HTL) of sewage sludge in a continuous flow pilot scale reactor at conditions expected to reflect future ...
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Extraction, isolation, structure elucidation and evaluation of toxicity, anti-inflammatory and analgesic activity of Pituranthos scoparius constituents [PDF]
The present work aimed to investigate an ethnobotanical survey about Pituranthos scoparius and assess the toxicity, anti-inflammatory (in vitro, and in vivo) potential, in vitro antioxidant, and analgesic effects of stems and roots of Pituranthos scoparius. Furthermore; to isolate and elucidate the chemical constituents of the n-butanol stem extract of
arxiv
Joint Distribution and Transitions of Pain and Activity in Critically Ill Patients [PDF]
Pain and physical function are both essential indices of recovery in critically ill patients in the Intensive Care Units (ICU). Simultaneous monitoring of pain intensity and patient activity can be important for determining which analgesic interventions can optimize mobility and function, while minimizing opioid harm. Nonetheless, so far, our knowledge
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Old Drugs for JAK-STAT Pathway Inhibition in COVID-19 [PDF]
The pandemic threat of COVID-19 with more than 37 million cases in which about 5 percent entering critical stage characterized by cytokine storm and hyperinflammatory condition, the state more often leads to admission to intensive care unit with rapid mortality.
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Can a microscopic stochastic model explain the emergence of pain cycles in patients? [PDF]
A stochastic model is here introduced to investigate the molecular mechanisms which trigger the perception of pain. The action of analgesic drug compounds is discussed in a dynamical context, where the competition with inactive species is explicitly accounted for.
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Binding Pathway of Opiates to $μ$ Opioid Receptors Revealed by Unsupervised Machine Learning [PDF]
Many important analgesics relieve pain by binding to the $\mu$-Opioid Receptor ($\mu$OR), which makes the $\mu$OR among the most clinically relevant proteins of the G Protein Coupled Receptor (GPCR) family. Despite previous studies on the activation pathways of the GPCRs, the mechanism of opiate binding and the selectivity of $\mu$OR are largely ...
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Caffeine Modulates the Dynamics of DODAB Membranes: Role of the Physical State of the Bilayer [PDF]
Caffeine (1,3,7-trimethylxanthine), an ingredient of coffee, is used worldwide as a psychostimulant, antioxidant, and adjuvant analgesic. To gain insights into the action mechanism of caffeine, we report on its effects on the phase behaviour and microscopic dynamics of a dioctadecyldimethylammonium bromide (DODAB) lipid membrane, as studied ...
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Stereotypical escape behavior in Caenorhabditis elegans allows quantification of nociceptive stimuli levels [PDF]
Experiments of pain with human subjects are difficult, subjective, and ethically constrained. Since the molecular mechanisms of pain transduction are reasonably conserved among different species, these problems are partially solved by the use of animal models. However, animals cannot easily communicate to us their own pain levels. Thus progress depends
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