• Dextrorphan is produced by O-demethylation of dextromethorphan by CYP2D6. (wikipedia.org)
  • Dextrorphan is an NMDA antagonist and contributes to the psychoactive effects of dextromethorphan. (wikipedia.org)
  • The pharmacology of dextrorphan is similar to that of dextromethorphan (DXM). (wikipedia.org)
  • Dextrorphan has a notably longer elimination half-life than its parent compound, and therefore has a tendency to accumulate in the blood after repeated administration of normally dosed dextromethorphan formulations. (wikipedia.org)
  • The pharmacological profile and regional distribution of [ 3 H]dextrorphan binding sites appear to distinguish these sites from those labeled either by [ 3 H]dextromethorphan or by putative σ receptor radioligands. (elsevier.com)
  • In contrast, the pharmacological signature and distribution of high affinity [ 3 H]dextrorphan binding sites in rat brain are incongruous with those of either the σ receptor or [ 3 H]dextromethorphan binding sites. (elsevier.com)
  • Accordingly, the interaction of dextrorphan and dextromethorphan at sites labeled by [ 3 H]dextrorphan, but not at sites labeled by [ 3 H]dextromethorphan or by σ ligands, adequately accounts for the anticonvulsant and neuroprotective efficacies of these compounds in vivo. (elsevier.com)
  • METHODS: CYP2D6 extensive metabolism was determined upon appropriate dextromethorphan/dextrorphan (DM/DX) urinary excretion ratios (≤0.30). (uzh.ch)
  • Furthermore, CYP2D6 metabolic activity was determined in a subset of 50 patients by assessing dextromethorphan/dextrorphan urinary excretion ratios. (uzh.ch)
  • However, dextrorphan is much more potent as an NMDA receptor antagonist as well much less active as a serotonin reuptake inhibitor, but retains DXM's activity as a norepinephrine reuptake inhibitor. (wikipedia.org)
  • Data from thoroughly washed forebrain membranes suggest that [ 3 H]dextrorphan predominantly labels a high affinity site defined by the activated state of the N-methyl-D-aspartate (NMDA) receptor-channel complex. (elsevier.com)
  • The critical relationship between [ 3 H]dextrorphan binding and activation of the NMDA receptor-complex is suggested by the profound dependence of [ 3 H]dextrorphan binding on glutamate in well washed membranes. (elsevier.com)
  • Basal specific [ 3 H]dextrorphan binding is nearly totally suppressed by the specific competitive NMDA antagonist D(-)-2-amino-5-phosphonopentanoic acid (D-AP5), in a glutamate- but not glycine-surmountable manner. (elsevier.com)
  • The NMDA receptor specificity of the modulation of [ 3 H]dextrorphan binding by glutamate and glycine is indicated by the sensitivity of their effects to competitive antagonism by D-AP5 and 3-amino-1-hydroxy-2-pyrrolidone (HA-966), respectively, and by the accordant rank orders of potency of glycine analogs as modulators of [ 3 H]dextrorphan binding and as ligands at the strychnine-insensitive glycine site. (elsevier.com)
  • The divalent cations Mg 2+ and Zn 2+ and the polyamines spermine and spermidine regulate [ 3 H]dextrorphan binding in a manner consistent with radioligand interaction at the noncompetitive NMDA antagonist domain. (elsevier.com)
  • Both 45Ca2+ accumulation and cell death could be attenuated in a dose-dependent manner by the competitive NMDA antagonist D-aminophosphonovalerate or the noncompetitive antagonist dextrorphan, with IC50 values of approximately 100 microM and 15 microM, respectively. (jneurosci.org)
  • The nonlinear kinetics of dextrorphan after iv administration appeared to occur only after potentially toxic dosing regimens of dextrorphan hydrochloride. (aspetjournals.org)
  • We postulate mechanisms to explain the dose- and time-dependent kinetics of dextrorphan observed in the beagle dog. (aspetjournals.org)
  • The kinetics of [ 3 H]dextrorphan binding in the presence of saturating concentrations of glutamate and glycine are complex and inadequately described by monoexponential association and dissociation processes. (elsevier.com)
  • We found that both DM and its metabolite dextrorphan block nicotinic receptor function in a noncompetitive but reversible manner, suggesting that both drugs block the receptor channel. (aspetjournals.org)
  • The AUC of the conjugated metabolites of dextrorphan decreased in a time-dependent manner for the 8.8 mg/kg/day dosing regimen. (aspetjournals.org)
  • Glutamate and glycine each stimulate [ 3 H]dextrorphan binding in a concentration-dependent manner, effecting maximal increases from control of up to 30-and 14-fold, respectively. (elsevier.com)
  • Levorphanol but not dextrorphan suppresses the foot-lifting response to an aversive thermal stimulus in the terrestrial snail, Cepaea nemoralis 的翻译是: 是什么意思?英文翻译中文,中文 (woyaofanyi.com)
  • Similar results have been obtained with levorphanol, dextrorphan (the optical isomer of levorphanol), levallorphan, and naloxone. (aspetjournals.org)
  • Since the same effects are obtained with narcotics (heroin, levorphanol), morphine antagonists (levallorphan, naloxone), and dextrorphan, which is inactive in man, it would appear that the antibacterial effects are not related to the effects of morphine derivatives in man. (aspetjournals.org)
  • and to Roche Products Ltd. for gifts of levorphanol, dextrorphan, and levallorphan. (aspetjournals.org)
  • Dextrorphan is produced by O-demethylation of dextromethorphan by CYP2D6. (wikipedia.org)
  • METHODS: CYP2D6 extensive metabolism was determined upon appropriate dextromethorphan/dextrorphan (DM/DX) urinary excretion ratios (≤0.30). (uzh.ch)
  • Furthermore, CYP2D6 metabolic activity was determined in a subset of 50 patients by assessing dextromethorphan/dextrorphan urinary excretion ratios. (uzh.ch)
  • Dextrorphan (DXO) is a psychoactive drug of the morphinan class which acts as an antitussive or cough suppressant and dissociative hallucinogen. (wikipedia.org)
  • Robertson said the horse received Dextrorphan, a cough suppressant, in an accidental contamination. (casino.org)
  • Another Baffert horse, Merneith, tested positive for the cough suppressant dextrorphan after racing last summer at Del Mar in California. (kxnet.com)
  • We found that both DM and its metabolite dextrorphan block nicotinic receptor function in a noncompetitive but reversible manner, suggesting that both drugs block the receptor channel. (aspetjournals.org)
  • For all dogs, however, dextrorphan plasma clearance approached or exceeded hepatic plasma flow rate, suggesting the possibility of extrahepatic metabolism or elimination. (aspetjournals.org)
  • Accumulating evidence suggests that metabolism to phencyclidine-like dextrorphan is not essential for the neuroprotective activity of dextromethorphan. (go.jp)
  • 1][2] It is an analogue of dextromethorphan and dextrorphan, but lacks significant NMDA receptor antagonistic action and dissociative effects, thereby having reduced abuse potential and adverse effects in comparison. (pearltrees.com)
  • Dextromethorphan and dextrorphan in saliva and urine were assayed by HPLC. (elsevier.com)
  • The AUC of the conjugated metabolites of dextrorphan decreased in a time-dependent manner for the 8.8 mg/kg/day dosing regimen. (aspetjournals.org)
  • One of its metabolites (which means a compound that is made after dextomethorphan is broken down by the body), dextrorphan, reaches its peak levels approximately 2 hours after the medication is taken. (livestrong.com)
  • As well, the metabolite 3-methoxymorphinan of dextrorphan (thus a second-level metabolite of DXM) produces local anesthetic effects in rats with potency above dextrorphan, but below that of DXM. (kitairu.net)
  • Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. (harvard.edu)
  • When 30 mg/(kg ip) dextrorphan was administered to male rats, neurotoxic changes were observed only 30 minutes post-dose. (wikipedia.org)
  • Dopamine enhancement of dextrorphan-induced skin antinociception in response to needle pinpricks in rats. (annals.org)
  • Accordingly, the interaction of dextrorphan and dextromethorphan at sites labeled by [ 3 H]dextrorphan, but not at sites labeled by [ 3 H]dextromethorphan or by σ ligands, adequately accounts for the anticonvulsant and neuroprotective efficacies of these compounds in vivo. (elsevier.com)
  • In contrast, the pharmacological signature and distribution of high affinity [ 3 H]dextrorphan binding sites in rat brain are incongruous with those of either the σ receptor or [ 3 H]dextromethorphan binding sites. (elsevier.com)
  • Upon multiple dosing, the plasma clearance of dextrorphan increased in a time-dependent fashion for the two highest doses, approaching values observed for the 0.88 mg/kg/day iv dosing regimen. (aspetjournals.org)
  • Plasma concentrations of dextromethorphan varied between 74-1730 ng/ml and its metabolite dextrorphan varied between 349-3790 ng/ml. (bmj.com)
  • Dextrorphan was under development for the treatment of stroke, and reached phase II clinical trials for this indication, but development was discontinued. (wikipedia.org)
  • Intrathecal treatment with dextrorphan or ketamine potently reduces pain-related behaviors in a rat model of peripheral mononeuropathy," Brain Research, 605: 164-168 (1993). (freepatentsonline.com)