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  • DPDPE
  • This evoked internalization was significantly reduced by morphine (60 nmol), DAMGO (1 nmol), and DPDPE (100 nmol), but not by the κ agonist trans -(1 S ,2 S )-3,4-dichloro- N -mathyl- N -[2-(1-pyrrolidinyl)cyclohexyl]-benzeneacetamide hydrochloride (200 nmol), delivered at spinal cord segment L2 using intrathecal catheters. (jneurosci.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)
  • naloxone
  • 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)
  • 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)
  • neurons
  • A dye (DiI), placed in small cavities drilled in rat molars ∼1 week before harvesting the trigeminal ganglia, is transported to the cell body, where its fluorescence distinguishes tooth-pulp afferents from other dissociated trigeminal sensory neurons (Fig. 2 ). (jneurosci.org)
  • In cultured mouse dorsal root ganglion neurons, two mechanistically different forms of desensitization were observed after acute or chronic treatment with the μ agonist [ d -Ala 2 , N- MePhe 4 , Gly-ol 5 ]-enkephalin (DAMGO). (jneurosci.org)
  • affinity
  • 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)
  • In vitro measures of opioid binding affinity ( K i ) and functional activity [EC 50 for agonist stimulated guanosine 5′- O -(3-[ 35 S]thio)triphosphate binding] and relevant clinical parameters were obtained to construct in vitro-to-preclinical and preclinical-to-clinical correlations. (aspetjournals.org)
  • The higher affinity type was designated μ 1 , and the lower affinity morphine-selective type was designated μ 2 ( 7 , 8 ). (jimmunol.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)
  • 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)
  • acute
  • 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)
  • membrane
  • 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)
  • 2 The activation of MORs result in reduction of 3′-5′-cyclic adenosine monophosphate, membrane hyperpolarization, and subsequent neuronal depression. (asahq.org)
  • basal
  • Our laboratory has demonstrated the presence of basal MOR signaling activity in various tissues in cell culture (Wang et al. (aspetjournals.org)
  • 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)
  • ketamine
  • 2 For instance, ketamine combined with morphine might be clinically efficient at lower doses than those currently used when administered separately. (asahq.org)
  • 4,5 Whether ketamine combined with morphine is a clinically relevant combination in orofacial pain is still unknown. (asahq.org)
  • 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)
  • 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)
  • 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)