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  • antagonist
  • In this study, we tested basal MOR-signaling activity in brain tissue from untreated and morphine-pretreated mice, in comparison to antagonist-induced withdrawal in morphine-dependent mice. (aspetjournals.org)
  • Second, morphine pretreatment affects the antagonist properties of naloxone and naltrexone. (aspetjournals.org)
  • 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)
  • analgesic
  • MORPHINE is a highly effective analgesic that has been used for centuries. (asahq.org)
  • 1 Because those adverse effects occur through the use of large doses of the drug, enormous effort has been invested to find a means of enhancing its analgesic efficacy and reducing undesirable side effects of morphine. (asahq.org)
  • IN contemporary medicine, the relief of moderate to severe pain is principally managed by treatment with opioid analgesic medication. (asahq.org)
  • Additionally, 3 developed analgesic tolerance more slowly than morphine, showed limited physical dependence, respiratory depression, constipation, and displayed no reward or aversion in CPP/CPA assays, suggesting that analogs might represent a promising new generation of novel pain relievers. (pubmedcentralcanada.ca)
  • The goal of this article is to evaluate the alterations that occur at the K ATP channel during morphine tolerance and physical dependence to ultimately determine whether openers of K ATP channels could be useful analgesic agents in patients who have undergone morphine therapy. (aspetjournals.org)
  • pretreatment
  • Using guanosine 5′- O -(3-[ 35 S]thio)triphosphate ([ 35 S]GTPγS) binding and adenylyl cyclase activity assay in brain homogenates, we demonstrated that morphine pretreatment of mice enhanced basal MOR signaling in mouse brain homogenates and, moreover, caused persistent changes in the effects of naloxone and naltrexone, antagonists that elicit severe withdrawal in dependent subjects. (aspetjournals.org)
  • Moreover, naloxone and naltrexone stimulated adenylyl cyclase activity in striatum homogenates only after morphine pretreatment, by reversing the inhibitory effects of basal MOR activity. (aspetjournals.org)
  • antinociception
  • Here we examine peripheral antinociception elicited by exogenously applied EM-1 and EM-2 and the contribution of EM-containing leukocytes to stress- and corticotropin-releasing factor (CRF)-induced antinociception. (jneurosci.org)
  • Both forms of antinociception were strongly attenuated by anti-β-endorphin and to a lesser degree by anti-EM-1 and anti-EM-2 antibodies injected into inflamed paws. (jneurosci.org)
  • rats
  • Thus, to test the proposed hypothesis, rats were treated with ketamine or morphine alone or with the combination of both drugs, and then submitted to the capsaicin orofacial test. (asahq.org)
  • In brains from heroin self-administering rats, decreased μ opioid-stimulated [ 35 S]GTPγS binding was observed in periaqueductal gray, locus coeruleus, lateral parabrachial nucleus, and commissural nucleus tractus solitarius, as previously observed in chronic morphine-treated animals. (jneurosci.org)
  • desensitization
  • Treatment with β-CNA after ME-induced desensitization decreased the absolute MOR-mediated current but did not inhibit recovery from desensitization. (aspetjournals.org)
  • 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)
  • Ser 375 phosphorylation was sufficient and required for morphine‐induced desensitization of MOR. (embopress.org)
  • Thus, morphine promotes terminal MOR desensitization by inducing a persistent modification of Ser 375 . (embopress.org)
  • antagonism
  • However, the significant reductions in deprivation-induced feeding following antisense probes directed against either exons 2, 4, 7, 8, or 13 of the MOP gene were modest compared with μ antagonism, suggesting a role for multiple μ-mediated mechanisms. (aspetjournals.org)
  • antagonists
  • Antagonists with inverse agonist property potentially have distinct treatment outcomes compared with neutral antagonists, i.e., antagonists that block agonist activation but do not affect basal activity. (aspetjournals.org)
  • Naloxone and naltrexone produce little effect per se in untreated cells, acting as neutral antagonists, whereas in morphine-pretreated cells, they exhibit inverse agonist effects that suppress basal MOR activity (Wang et al. (aspetjournals.org)
  • 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)
  • potency
  • 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)
  • drugs
  • GPCRs account for up to 50% of currently marketed drugs [ 1 - 4 ] and continue to be the focus of intense research in drug development. (stonel.info)
  • analgesia
  • 1,2 To minimize such undesirable effects, the clinical concept of balanced or multimodal analgesia proposes to use a combination of analgesics to provide better pain relief and to minimize the side effects of each drug. (asahq.org)
  • 10 Opioid analgesia may also affect other aspects of the immune response: morphine inhibits production of proinflammatory cytokines by monocytes and inhibits interleukin-2 transcription in activated T lymphocytes. (asahq.org)
  • naloxone
  • After cessation of morphine treatment, the time course of inverse naloxone effects on basal MOR signaling was similar to the time course of naltrexone-stimulated narcotic withdrawal over several days. (aspetjournals.org)
  • laboratory
  • Our laboratory has demonstrated the presence of basal MOR signaling activity in various tissues in cell culture (Wang et al. (aspetjournals.org)
  • ligand
  • 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)
  • doses
  • In contrast, morphine delivered by percutaneous injections at S1-S2 had only a modest effect on thermal escape, even at higher doses. (jneurosci.org)
  • 2 For instance, ketamine combined with morphine might be clinically efficient at lower doses than those currently used when administered separately. (asahq.org)
  • hyperpolarization
  • 2 The activation of MORs result in reduction of 3′-5′-cyclic adenosine monophosphate, membrane hyperpolarization, and subsequent neuronal depression. (asahq.org)
  • naltrexone
  • In morphine-treated monkeys discriminating naltrexone, thienorphine, and U50,488 neither substituted for nor modified the naltrexone discriminative stimulus. (aspetjournals.org)