Results 11 to 20 of about 30,638 (285)
Biomolecules, 2020 The peptide AVFQHNCQE demonstrated to produce nitric oxide-mediated antihypertensive effect. This study investigates the bioavailability and the opioid-like activity of this peptide after its oral administration.
Anna Mas-Capdevila +5 more
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Current Medicinal Chemistry, 2016 For decades the opioid receptors have been an attractive therapeutic target for the treatment of pain. Since the first discovery of enkephalin, approximately a dozen endogenous opioid peptides have been known to produce opioid activity and analgesia, but their therapeutics have been limited mainly due to low blood brain barrier penetration and poor ...
Michael Remesic +2 more
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Molecules, 2020 The macrocyclic tetrapeptide cyclo[Phe-d-Pro-Phe-Trp] (CJ-15,208) and its stereoisomer cyclo[Phe-d-Pro-Phe-d-Trp] exhibit different opioid activity profiles in vivo.
Ariana C. Brice-Tutt +7 more
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Molecules, 2020 The mu opioid receptor (MOR) is the primary target for analgesia of endogenous opioid peptides, alkaloids, synthetic small molecules with diverse scaffolds, and peptidomimetics.
Maria Dumitrascuta +4 more
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Protective Role and Functional Engineering of Neuropeptides in Depression and Anxiety: An Overview
Bioengineering, 2023 Behavioral disorders, such as anxiety and depression, are prevalent globally and touch children and adults on a regular basis. Therefore, it is critical to comprehend how these disorders are affected.
Nathalie Okdeh +7 more
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Molecules, 2021 Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists
Yusuke Karasawa +12 more
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Non-Opioid Peptides Targeting Opioid Effects [PDF]
International Journal of Molecular Sciences, 2021 Opioids are the most potent widely used analgesics, primarily, but not exclusively, in palliative care. However, they are associated with numerous side effects, such as tolerance, addiction, respiratory depression, and cardiovascular events. This, in turn, can result in their overuse in cases of addiction, the need for dose escalation in cases of ...
Katarzyna Kaczyńska +1 more
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LP1 and LP2: Dual-Target MOPr/DOPr Ligands as Drug Candidates for Persistent Pain Relief
Molecules, 2021 Although persistent pain is estimated to affect about 20% of the adult population, current treatments have poor results. Polypharmacology, which is the administration of more than one drug targeting on two or more different sites of action, represents a ...
Lorella Pasquinucci +5 more
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Discovery of Kynurenines Containing Oligopeptides as Potent Opioid Receptor Agonists
Biomolecules, 2020 Kynurenine (kyn) and kynurenic acid (kyna) are well-defined metabolites of tryptophan catabolism collectively known as “kynurenines”, which exert regulatory functions in host-microbiome signaling, immune cell response, and neuronal ...
Edina Szűcs +9 more
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High-affinity naloxone binding to filamin a prevents mu opioid receptor-Gs coupling underlying opioid tolerance and dependence. [PDF]
PLoS ONE, 2008 Ultra-low-dose opioid antagonists enhance opioid analgesia and reduce analgesic tolerance and dependence by preventing a G protein coupling switch (Gi/o to Gs) by the mu opioid receptor (MOR), although the binding site of such ultra-low-dose opioid ...
Hoau-Yan Wang +2 more
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