• Further lending credence to the exorphin dysfunction hypothesis are studies using "mixed agonist/antagonists" drugs (e.g., cyclazocine and nalorphine) that artificially stimulate and suppress the body's endorphin receptors and have been known to produce profound dysphoria bordering on psychosis in patients. (thefreedictionary.com)
  • Gluten therefore, by its "molecular mimicry" of endorphins (and enkephalins) reacts with the brain's endorphin receptors in the same deleterious way as cyclazocine or nalorphine. (thefreedictionary.com)
  • Haertzen, C. A.: Subjective effects of narcotic antagonists cyclazocine and nalorphine on the Addiction Research Centre Inventory (ARCI). (springer.com)
  • Both cyclazocine and nalorphine inhibit cAMP accumulation in COS-7 cells stably expressing the clone. (aspetjournals.org)
  • Morphine stimulus properties did not generalize to nalorphine or cyclazocine, which produce dissimilar subjective effects. (meta.org)
  • The stimulus properties of LSD generalized partially to cyclazocine, but not to nalorphine. (meta.org)
  • In humans cyclazocine and nalorphine produce a high incidence of psychotomimetic effects, but the subjective effects of cyclazocine are differentiable from those of LSD. (meta.org)
  • The agonist/antagonists, butorphanol and cyclazocine, when injected, behaved like kappa agonists and increased plasma corticosterone levels potently. (aspetjournals.org)
  • Their dysphoric actions observed with the kappa agonist cyclazocine are thought to be mediated by an action at sigma-phencyclidine receptors. (erowid.org)
  • Increasing the training dose of morphine shifted the morphine gradient to the right, increased the antagonist effects of cyclazocine and of l-NANM, and decreased their agonist effects, but did not alter the effects of ketamine. (umich.edu)
  • Benzomorphans I-cyclorphan(3a) Mu-antagonist girlfriend agonist dextromethorphan HO HJ O Cyclazocine (2) Cheap Mastigra 100mg In UK 2033 Bremazocine o HO Fig. (obyxova.ru)
  • A psychiatrist who has had experience with both methadone and antagonist maintenance programs contrasts 'the relaxed, jovial atmosphere of a methadone ward,' where patients are free of the postaddiction syndrome, with 'the tension, frustration, and anxiety that characterize a cyclazocine ward. (druglibrary.org)
  • Specific [ 3 H]phencyclidine binding can be displaced by cyclazocine (IC 50 = 350 nM) and by related benzomorphans, but not by classical opiates such as morphine or naloxone. (elsevier.com)
  • The generalization gradient of cyclazocine and of l-NANM, but not that of ketamine, was less steep than the gradient of morphine. (umich.edu)
  • Cyclazocine and l-NANM, but not U50,488 and ketamine, antagonized partially the discriminative stimulus (DS) effects of morphine. (umich.edu)
  • The full generalization produced by cyclazocine when the training dose of morphine was lowered could be blocked completely by naltrexone and l-NANM, but not by ketamine. (umich.edu)
  • These results suggest that cyclazocine and l-NANM, but not ketamine, produced partial generalization because of their low efficacy at the receptor that underlies the DS effects of morphine. (umich.edu)
  • 1986 Human psychopharmacology of ketocyclazocine as compared with cyclazocine, morphine and placebo. (takecarehomehealth.com)
  • Selective blockade of an excitatory synapse in rat cerebral cortex by the sigma opiate cyclazocine: an intracellular, in vitro study. (semanticscholar.org)
  • article{Thomson1985SelectiveBO, title={Selective blockade of an excitatory synapse in rat cerebral cortex by the sigma opiate cyclazocine: an intracellular, in vitro study. (semanticscholar.org)
  • In isolated slices of rat cortex, intracellularly recorded responses of pyramidal neurones to N-methylaspartate (NMA) and glutamate and responses to stimulation of the underlying white matter were compared and challenged with the sigma opiate cyclazocine. (semanticscholar.org)
  • Interaction of the psychotomimetic opiate cyclazocine with multiple receptor sites has been demonstrated biochemically. (elsevier.com)
  • Jaffe, J. H., Brill, L.: Cyclazocine, a long acting narcotic antagonist: its voluntary acceptance as a treatment modality by narcotics abusers. (springer.com)
  • Claim 1 of auxiliary request IIc differs from claim 1 of auxiliary request IIb in that the feature 'and wherein the opioid antagonist is selected from the group consisting of naloxone, nalmephene, cyclazocine, levallorphan, naltrexone and mixtures thereof' has been added. (epo.org)
  • 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine. (nih.gov)
  • Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. (nih.gov)
  • Research during the 1960s and 1970s into the possible use of cyclazocine for management of pain, and later for assisting treatment of narcotic addiction was severely hampered by the drug's psychotomimetic, dysphoric, and hallucinatory effects. (wikipedia.org)
  • Related drugs include phenazocine, dezocine, cyclazocine and several chemicals used in research on the central nervous system. (dbpedia.org)
  • Cyclazocine (2.5 mg/kg) and LSD (1.0 mg/kg) induced strikingly similar behavioural disruptions on well-established discriminated (Sidman) avoidance performance in rats. (springer.com)
  • The effects of cyclazocine and LSD in rats may be mediated through similar mechanisms. (springer.com)
  • The most recent study of cyclazocine, reported in the International Journal of the Addiction, 3 in 1971, indicates that of 186 addicts offered cyclazocine, 33 accepted, of whom 11 were believed to be abstinent twenty months later. (druglibrary.org)
  • Competition analyses involving rank order determinations for a series of opiates and other drugs indicate that the cyclazocine binding sites represent, in order of decreasing affinity, the classical opiate receptor (the putative 'μ' receptor), a second as yet uncharacterized opiate binding site, and the specific [ 3 H]phencyclidine binding site. (elsevier.com)
  • Cyclazocine has been postulated to interact with μ, κ, and σ opiate receptors (Martin et al. (elsevier.com)
  • The high- and low-affinity [ 3 H]cyclazocine sites exhibit differential sensitivities to sodium and also to the selective sulfhydryl reagent N-ethylmaleimide. (elsevier.com)
  • Replacement of the phenolic hydroxyl group in non-peptide opiates with the −CONH 2 group had previously been shown to result in compounds retaining high μ receptor binding affinity 5 , 6 and introduction of a (4'-phenyl)-phenethyl substituent at the −CONH 2 group of 8-carboxamido-cyclazocine did not diminish μ receptor binding affinity. (pubmedcentralcanada.ca)
  • D-EKC and D-cyclazocine, which bind to sigma sites, had no effect on corticosterone. (aspetjournals.org)
  • Research into the use of cyclazocine for the treatment of bipolar patients with depression was undertaken by Fink and colleagues (1970). (wikipedia.org)
  • The study suggests, but does not prove, that the few patients who accept cyclazocine do significantly better than similar patients who attempt abstinence without cyclazocine. (druglibrary.org)
  • "Cyclazocine revisited - Neurochemical Research" 21 (11). (wikipedia.org)