Receptors, Phencyclidine
Specific sites or molecular structures on cell membranes or in cells with which phencyclidine reacts or to which it binds to elicit the specific response of the cell to phencyclidine. Studies have demonstrated the presence of multiple receptor sites for PCP. These are the PCP/sigma site, which binds both PCP and psychotomimetic opiates but not certain antipsychotics, and the PCP site, which selectively binds PCP analogs.
Phenazocine
Nalorphine
Pentazocine
Dictionaries as Topic
Naloxone
Hallucinations
Hydromorphone
Hydrocodone
Oxymorphone
An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)
Analgesics, Opioid
Miosis
Codeine
Organophosphonates
Amination
Molecular Structure
Phosphorus
Structure-Activity Relationship
Stereoisomerism
Euphoria
Substance Abuse Treatment Centers
Methadone
Narcotics
Encyclopedias as Topic
MedlinePlus
Consumer Health Information
Social Media
Dissent and Disputes
Internet
Peer Review
An organized procedure carried out by a select committee of professionals in evaluating the performance of other professionals in meeting the standards of their specialty. Review by peers is used by editors in the evaluation of articles and other papers submitted for publication. Peer review is used also in the evaluation of grant applications. It is applied also in evaluating the quality of health care provided to patients.
Neuritis
Juxtaglomerular Apparatus
A complex of cells consisting of juxtaglomerular cells, extraglomerular mesangium lacis cells, the macula densa of the distal convoluted tubule, and granular epithelial peripolar cells. Juxtaglomerular cells are modified SMOOTH MUSCLE CELLS found in the walls of afferent glomerular arterioles and sometimes the efferent arterioles. Extraglomerular mesangium lacis cells are located in the angle between the afferent and efferent glomerular arterioles. Granular epithelial peripolar cells are located at the angle of reflection of the parietal to visceral angle of the renal corpuscle.
Vertigo
An illusion of movement, either of the external world revolving around the individual or of the individual revolving in space. Vertigo may be associated with disorders of the inner ear (EAR, INNER); VESTIBULAR NERVE; BRAINSTEM; or CEREBRAL CORTEX. Lesions in the TEMPORAL LOBE and PARIETAL LOBE may be associated with FOCAL SEIZURES that may feature vertigo as an ictal manifestation. (From Adams et al., Principles of Neurology, 6th ed, pp300-1)
Half-Life
Carbolines
Hyperthyroidism
Urinary Incontinence, Urge
Drug Labeling
Use of written, printed, or graphic materials upon or accompanying a drug container or wrapper. It includes contents, indications, effects, dosages, routes, methods, frequency and duration of administration, warnings, hazards, contraindications, side effects, precautions, and other relevant information.
Drugs, Generic
Safety-Based Drug Withdrawals
United States Food and Drug Administration
Leiomyoma
8-Carboxamidocyclazocine: a long-acting, novel benzomorphan. (1/42)
To obtain benzomorphans with a longer duration of action that may be potential therapeutics for treating cocaine abuse, 8-carboxamidocyclazocine was synthesized. The pharmacological properties of 8-carboxamidocyclazocine were compared with the parent compound cyclazocine. Changing the 8-hydroxyl group on cyclazocine to an 8-carboxamido group resulted in only a 2-fold decrease in the affinity of the compound for the kappa-receptor, and no change in the affinity for the mu-opioid receptor, with both compounds having K(i) values of less than 1 nM, based on radioligand binding assays. In the guanosine 5'-O -(3-[(35)S]thio)triphosphate ([(35)S]GTPgammaS) binding assay, the two compounds produced moderate stimulation of GTP binding to the human kappa- and mu-receptors. When given by i.c.v. injection, the compounds produced less than 60% antinociception in the mouse 55 degrees C warm-water tail-flick test. However, in the mouse writhing test, the compounds had high potency in producing antinociception. Antinociception induced by either 8-carboxamidocyclazocine or cyclazocine was mediated by both kappa- and mu-opioid receptors. Cyclazocine acted as a mu-antagonist in addition to its agonist properties at the mu-receptor, as measured by the inhibition of morphine-induced antinociception. In contrast, 8-carboxamidocyclazocine did not inhibit morphine-induced antinociception, demonstrating that it was not a mu-opioid receptor antagonist in this assay. An i.p. injection of an ED(70) dose of 8-carboxamidocyclazocine produced antinociception that lasted for 15 h in contrast to cyclazocine, which produced antinociception, lasting 2 h. 8-Carboxamidocyclazocine is a novel, long-acting benzomorphan, which possesses pharmacological properties that are distinct from the properties of cyclazocine. (+info)Neuroprotective effects of SKF 10,047 in cultured rat cerebellar neurons and in gerbil global brain ischemia. (2/42)
BACKGROUND AND PURPOSE: Excitatory amino acids and their receptors are involved in mediating ischemic neuronal damage. The sigma-agonists are believed to interact with the N-methyl-D-aspartate receptor. Therefore, we studied the neuroprotective, hypothermic, and motor deficit effects of the sigma-agonist SKF 10,047 and the N-methyl-D-aspartate antagonist MK-801. METHODS: Neuroprotective effects were compared using an in vitro ischemia model of cultured rat cerebellar granule cells and the gerbil model of global brain ischemia induced by 5 minutes of bilateral carotid artery occlusion followed by 7 days of reperfusion. RESULTS: In vitro, (+)MK-801 protected against 100 microM glutamate with a 50% protective concentration of 30 nM, followed by (-)MK-801 (150 nM), cyclazocine (0.5 microM), (+)SKF 10,047 (3.3 microM), pentazocine (5 microM), and (-)SKF 10,047 (10 microM). In vivo, (+)SKF 10,047 pretreatment (60 mg/kg) or multiple postischemic treatments provided neuroprotection comparable with MK-801 pretreatment (10 mg/kg). When ischemic animals were administered the multiple dosing regimen of (+)SKF 10,047, no hypothermic effect was noted in the temporalis muscle over 4 hours' postischemia. Motor deficits monitored by a swing grid test showed that 50% recovery from (+)SKF 10,047 was 5.5 times faster than recovery from MK-801. CONCLUSIONS: These results are the first to report a hypothermia-free, in vivo neuroprotective effect of (+)SKF 10,047, a prototypical drug of the sigma-agonist class. (+info)Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC. (3/42)
A series of aryl-containing N-monosubstituted analogues of the lead compound 8-[N-((4'-phenyl)-phenethyl)]-carboxamidocyclazocine were synthesized and evaluated to probe a putative hydrophobic binding pocket of opioid receptors. Very high binding affinity to the mu opioid receptor was achieved though the N-(2-(4'-methoxybiphenyl-4-yl)ethyl) analogue of 8-CAC. High binding affinity to mu and very high binding affinity to kappa opioid receptors was observed for the N-(3-bromophenethyl) analogue of 8-CAC. High binding affinity to all three opioid receptors were observed for the N-(2-naphthylethyl) analogue of 8-CAC. (+info)Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine. (4/42)
(+info)Effects of eptazocine, a novel analgesic, on KCN-induced changes in the cerebral contents of glycolytic metabolites and high-energy phosphates in mice. (5/42)
Effects of eptazocine on cerebral metabolic changes due to a sublethal dose of KCN were investigated in mice. KCN (2 mg/kg, i.v.) induced a temporary loss of consciousness being moderated by eptazocine (1-10 mg/kg) in a dose-dependent manner. The KCN injection decreased the contents of phosphocreatine (PCr), ATP and glucose and increased the contents of AMP and lactate, resulting in a 34% decrease in energy charge potential (ECP) and an increase in lactate/pyruvate (L/P) ratio. Such changes were improved by eptazocine (10 mg/kg) and EKC (3 mg/kg), but not by pentazocine (10 mg/kg) and morphine (3 mg/kg), and the improving effect of eptazocine was completely inhibited by MR-2266 (3 mg/kg), a relatively selective opioid kappa-receptor antagonist. On the other hand, eptazocine (3, 10 mg/kg) was found to increase the glucose content in normal mice, but not to give significant changes in the contents of glycolytic metabolites and high-energy phosphates. These results suggest that eptazocine may improve anoxic changes in cerebral energy metabolism. (+info)Binding of opioids to human MCF-7 breast cancer cells and their effects on growth. (6/42)
The well characterized human breast cancer cell line, MCF-7, has been shown to possess membrane receptors for various opioid ligands, and these compounds have been shown to modulate the growth of the cells in culture. Using specific radioligands for the receptor types, we were able to demonstrate that the MCF-7 cells possess multiple opioid receptor types. Relatively high-affinity-binding sites are present for the mu- and kappa-specific ligands, while lower affinity sites are present for the delta-agonist. Opioid ligands specific for the different receptor types significantly inhibited the growth of the MCF-7 cells in a dose-dependent manner when grown in the presence of 10% fetal bovine serum. This inhibitory effect was reversed by the simultaneous administration of the opioid receptor antagonist, naloxone. However, the opioid effect appears to be restricted to the hormonally responsive fraction of the MCF-7 cell growth. Cells grown in the presence of charcoal-stripped fetal bovine serum are refractory to the effects of the opioids unless the media is supplemented with estradiol. The data presented here suggest an important regulatory role for opioids in the growth and development of human breast cancers. (+info)Opioid receptor ligands in the neonatal rat spinal cord: binding and in vitro depression of the nociceptive responses. (7/42)
1. Opioid receptors in the neonatal rat spinal cord have been characterized by measurements of ligand binding to crude membrane fractions and by functional tests on the nociceptive spinal response in a spinal cord-tail preparation in vitro. 2. There were high affinity binding sites for [3H]-[D-Ala2, MePhe4, Gly(ol)5]enkephalin (DAGOL), [3H]-U69593, and [3H]-ethylketocyclazocine (EKC) on spinal cord membranes from neonatal rats. Hill slopes for binding of [3H]-DAGOL and [3H]-U69593 were close to unity. The Hill slope for binding of [3H]-EKC was less than unity, even after its interactions at mu-receptors had been blocked with 100 nM unlabelled DAGOL. Binding sites for [3H]-[D-Pen2, D-Pen5]enkephalin (DPDPE) could not be detected. 3. In competition assays U50488 was as potent as PD117302 and U69593 in competition for either [3H]-U69593 or [3H]-EKC binding sites. Hill slopes for a range of competing ligands at [3H]-DAGOL or [3H]-U69593 sites were close to unity. Hill slopes for competition at [3H]-EKC sites were less than one. 4. In the spinal cord-tail preparation from neonatal rats, opioid receptor agonists depressed spinal nociceptive responses evoked by application of capsaicin or heat to the tail. The order of potency was DAGOL greater than U69593 = PD117302 greater than morphine greater than U50488 = [D-Pen2, L-Pen5]enkephalin (DPLPE). 5. The antagonist naloxone was about equally potent against DAGOL, morphine and DPLPE, and about ten times less potent against U69593 and PD117302. The effects of U50488 were much less sensitive to blockade by naloxone than the effects of PD11703 or U69593. The Kappa antagonist, nor-binaltorphimine was equipotent against all three Kappa agonists. 6. The absence of delta-binding sites, and the low potency and relatively high sensitivity to naloxone suggest that DPLPE could be working at mu-receptors in the neonatal rat spinal cord. 7. The binding assays show that U50488 has the same affinity as PD1 17302 and U69593 for Kappa-receptors, yet it was less effective in the depression of nociceptive responses. This may be because U50488 has a relatively low efficacy at Kappa-receptors. It is possible that at high concentrations U50488 activates receptors not affected by other Kappa-ligands. These additional receptors may be non-opioid receptors (hence the insensitivity to naloxone), or they could be a subtype of Kappa-opioid receptor. (+info)On the mechanism by which midazolam causes spinally mediated analgesia. (8/42)
The electrical current thresholds for pain (ECTP) in the skin of the neck and tail were measured in rats with chronically implanted lumbar subarachnoid catheters. The effects of a benzodiazepine antagonist and a gamma-aminobutyric acid (GABA) antagonist on the analgesic effects of equivalent doses of midazolam, fentanyl, and ketocyclazocine were studied. These were the minimum doses producing maximal segmental analgesia when given intrathecally (i.e., they all caused a significant and maximum increase in ECTP in the tail, which was similar for all three drugs, but no significant change in the ECTP in the neck). Flumazenil (Ro 15-1788) administration caused a parallel shift to the right of the dose-response curve for midazolam spinal analgesia. Segmental analgesia following midazolam was also significantly attenuated (P less than 0.05) when the selective GABA antagonist bicuculline was given intrathecally at the same time as midazolam. The highest dose of bicuculline used (50 pmol) caused no significant attenuation of the segmental analgesic effects of either ketocyclazocine or fentanyl. The authors concluded that the segmental analgesia produced by intrathecal midazolam is mediated by the benzodiazepine-GABA receptor complex that is involved in other benzodiazepine actions. (+info)
Cyclazocine - definition of cyclazocine by The Free Dictionary
A correlative evaluation of cyclazocine, LSD and naloxone on continuous discriminated avoidance in rats | SpringerLink
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Pentazocine6
- Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. (wikipedia.org)
- These include cyclazocine, pentazocine, and phenazocine. (wikipedia.org)
- The narcotic analgesics morphine, codeine, meperidine and methadone and the narcotic antagonist analgesics cyclazocine, cyclorphan, nalorphine and pentazocine were active. (aspetjournals.org)
- NARCAN (naloxone) is indicated for the complete or partial reversal of opioid depression, including respiratory depression, induced by natural and synthetic opioids, including propoxyphene, methadone and certain mixed agonist-antagonist analgesics: nalbuphine, pentazocine, butorphanol, and cyclazocine. (rxlist.com)
- They are distinguished from sigma2 receptors as they have high affinity and stereoselectivity for the (+)-isomers of pentazocine, SK&F 10047 and cyclazocine, and different subcellular localizations. (genecards.org)
- f)cyclazocine, and (-)pentazocine and also for some narcoleptics such as haloperidol. (allindianpatents.com)
Nalorphine7
- 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)
Agonist4
- 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)
Methadone1
- 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)
Morphine6
- 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)
Opiate cyclazocine4
- 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)
Long acting narcotic ant1
- Jaffe, J. H., Brill, L.: Cyclazocine, a long acting narcotic antagonist: its voluntary acceptance as a treatment modality by narcotics abusers. (springer.com)
Naloxone1
- 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)
Opioid2
Psychotomimetic1
- 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)
Dezocine1
- Related drugs include phenazocine, dezocine, cyclazocine and several chemicals used in research on the central nervous system. (dbpedia.org)
Rats2
- 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)
Addiction1
- 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)
Phencyclidine1
- 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)
Receptors1
- Cyclazocine has been postulated to interact with μ, κ, and σ opiate receptors (Martin et al. (elsevier.com)
Affinity2
- 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)
Sigma1
- D-EKC and D-cyclazocine, which bind to sigma sites, had no effect on corticosterone. (aspetjournals.org)
Fink1
- Research into the use of cyclazocine for the treatment of bipolar patients with depression was undertaken by Fink and colleagues (1970). (wikipedia.org)
Study1
- 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)
Research1
- "Cyclazocine revisited - Neurochemical Research" 21 (11). (wikipedia.org)