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  • peptide
  • Endomorphin-1 and endomorphin-2 were synthesized at our institution's Microchemistry Facility, purified by high-performance liquid chromatography, their structures verified by mass spectroscopy and the peptide content (58% for endomorphin-1 and 74% for endomorphin-2) determined by Rockefeller University's Protein Technology Center. (aspetjournals.org)
  • 3. The method of claim 2, wherein said peptide has a binding affinity for the kappa opioid receptor that is 10 times greater, 100 times greater, 1,000 times greater, or more than its binding affinity for non-kappa opioid receptors. (patentsencyclopedia.com)
  • The present study in Sprague Dawley rats examined the possibility that the orexigenic peptide systems, enkephalin (ENK) and orexin (OX), which are stimulated by nicotine in adult animals and promote consummatory behavior, may be similarly responsive to nicotine's stimulatory effect in utero while having long-term behavioral consequences. (jneurosci.org)
  • 2017
  • Thirty-three new synthetic opioids were detected in Europe between 2009 and 2017 ( 5 ). (aaccjnls.org)
  • leucine
  • Although related to each other, the sequences of endomorphin-1 (Tyr-Pro-Trp-Phe-NH 2 ) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH 2 ) are quite distinct from traditional opioids in which the first four amino acids are Tyr-Gly-Gly-Phe followed by either methionine or leucine. (aspetjournals.org)
  • 2002
  • and some studies suggested that exogenous EM-2-induced antinociception was mediated by the release of dynorphin A(1-17) and methionine (Met)-enkephalin, which activated κ- and δ-receptors, respectively ( Tseng, 2002 ). (jneurosci.org)
  • Pharmacology
  • 6-Cyano-7-nitroquinoxaline-2,3-dione--pharmacology;Analysis of Variance;Behavior, Addictive--physiopathology;Conditioning, Operant--drug effects;Cues;Dopamine Antagonists--pharmacology;Dose-Response Relationship, Drug;Excitatory Amino Acid. (musc.edu)
  • antagonist
  • demonstrated that deprivation-induced feeding in rats was maximally reduced by an AS ODN probe directed against exon 2 of the KOP gene, an effect complementary to κ antagonist effects, whereas probes directed against exons 2, 3, or 4 of the MOP gene, exon 1 of the DOP gene, and exon 1 of the NOP gene resulted in modest reductions in deprivation-induced intake. (aspetjournals.org)
  • In assays measuring G-protein activation, TIPP failed to stimulate guanosine 5′- O -(3-[ 35 S]thio)triphosphate ([ 35 S]GTPγS) binding in membrane preparations, which is consistent with an antagonist profile. (aspetjournals.org)
  • neurons
  • A prominent example is the inhibition of (pronociceptive) substance P release from primary afferent sensory neurons in the spinal cord and from their peripheral terminals (Kondo et al. (damasgate.com)
  • Laboratory
  • Our laboratory has demonstrated the presence of basal MOR signaling activity in various tissues in cell culture (Wang et al. (aspetjournals.org)
  • opioids
  • From an additional 10 samples found to contain other opioids, 5 were correctly scored positive. (aaccjnls.org)
  • In Europe and North America, highly potent synthetic opioids, which mimic the effects of heroin and morphine, are a growing health threat ( 1 - 4 ). (aaccjnls.org)
  • These synthetic opioids were initially explored by research groups or pharmaceutical companies for their potential medicinal use, but they have recently found their way to the illicit drug market ( 1 - 4 ). (aaccjnls.org)
  • These new synthetic opioids are a major public health concern owing to their high potency, ease of accessibility over the internet, and distribution into the regular street heroin supply, where they are often mixed with or substituted for heroin, leading to life-threatening respiratory depression and death ( 1 - 4 ). (aaccjnls.org)
  • 2-4 Although the occurrence of severe respiratory depression and related deaths in the treatment of acute and perioperative pain seems constant over the years (with an incidence of at least 0.5%), 1 , 5 over the last decade there has been a dramatic surge in fatalities from prescription opioids in chronic pain patients due to a dramatic increase in opioid consumption. (asahq.org)
  • desensitization
  • B, β-CNA (500 nM, 2 min) was applied immediately after ME (30 μM, 10 min) induced desensitization, and recovery was again measured with ME test pulses at 5 and 45 min. (aspetjournals.org)
  • hyperpolarization
  • 2 The activation of MORs result in reduction of 3′-5′-cyclic adenosine monophosphate, membrane hyperpolarization, and subsequent neuronal depression. (asahq.org)
  • membrane
  • TM residues within the lipophilic environment of the cell membrane are key in ligand recognition and/or signal transduction and are expected to be oriented toward a relatively hydrophilic central cavity (Surratt et al. (damasgate.com)
  • proteins
  • In general, fast activation of ERKs (2 min) mediated by G proteins resulted in the nuclear translocation of phosphorylated ERKs, whereas a slower activation of ERKs (10 min) mediated by β-arrestins resulted in the cytosolic retention of the phosphorylated ERKs. (aspetjournals.org)
  • stimulation
  • Affinity and potency were determined using radioligand displacement and stimulation of guanosine 5′- O -(3-[ 35 S]thio)triphosphate binding in C6 (μ, δ) and Chinese hamster ovary (κ) cell membranes. (aspetjournals.org)
  • tissues
  • Pain, an unpleasant experience caused by intense or damaging stimuli, is primarily protective in nature and can act as a sensorial modality to indicate the presence of tissues injury [ 1 , 2 ]. (hindawi.com)