An analgesic with mixed narcotic agonist-antagonist properties.
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.
An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)
A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.
The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)
A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).
An effect usually, but not necessarily, beneficial that is attributable to an expectation that the regimen will have an effect, i.e., the effect is due to the power of suggestion.
A peptide, of about 33 amino acids, secreted by the upper INTESTINAL MUCOSA and also found in the central nervous system. It causes gallbladder contraction, release of pancreatic exocrine (or digestive) enzymes, and affects other gastrointestinal functions. Cholecystokinin may be the mediator of satiety.
Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.

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)

Stomach ulcers are caused by an imbalance between the acid and mucus in the stomach, which can lead to inflammation and damage to the stomach lining. Factors that can contribute to the development of a stomach ulcer include:

* Infection with the bacterium Helicobacter pylori (H. pylori)
* Overuse of nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen, and naproxen
* Excessive alcohol consumption
* Smoking
* Stress
* Zollinger-Ellison syndrome, a rare condition that causes the stomach to produce too much acid.

Symptoms of a stomach ulcer may include:

* Pain in the upper abdomen, often described as a burning or gnawing sensation
* Nausea and vomiting
* Bloating and gas
* Abdominal tenderness
* Loss of appetite
* Weight loss

Treatment for stomach ulcers typically involves antibiotics to kill H. pylori, if present, and acid-suppressing medications to reduce the amount of acid in the stomach. In severe cases, surgery may be necessary. Lifestyle changes, such as avoiding NSAIDs, alcohol, and smoking, can also help manage symptoms and prevent recurrence.

Preventive measures for stomach ulcers include:

* Avoiding NSAIDs and other irritating substances
* Using acid-suppressing medications as needed
* Maintaining a healthy diet and lifestyle
* Managing stress
* Avoiding excessive alcohol consumption

It is important to seek medical attention if symptoms persist or worsen over time, as stomach ulcers can lead to complications such as bleeding, perforation, and obstruction. Early diagnosis and treatment can help prevent these complications and improve outcomes.

... is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs ... Research during the 1960s and 1970s into the possible use of cyclazocine for management of pain, and later for assisting ... Freedman, A. M.; Fink, M.; Sharoff, R.; Zaks, A. (1967). "Cyclazocine and Methadone in Narcotic Addiction". The Journal of the ... Research into the use of cyclazocine for the treatment of bipolar patients with depression was undertaken by Fink and ...
These include cyclazocine, pentazocine, and phenazocine. The fully saturated analog of azocine is azocane. Azocine rings are ...
Cyclazocine (hallucinogenic) Volazocine Stitzel RE (2004). Modern pharmacology with clinical applications (6th ed.). ...
Benzomorphan ketazocine cyclazocine World Health Organization (2004). "The use of stems in the selection of International ...
Similarly to cyclazocine, 8-CAC acts as an agonist at both the μ and κ opioid receptors, but has a much longer duration of ... Unexpectedly it was discovered that the phenolic hydroxyl group of cyclazocine could be replaced by a carboxamido group with ... 8-Carboxamidocyclazocine (8-CAC) is an opioid analgesic drug related to cyclazocine, discovered by medicinal chemist Mark P. ... Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine". Bioorganic & Medicinal Chemistry Letters. ...
... cyclazocine, and dextrorphan in the pigeon". Psychopharmacology. 73 (3): 286-91. doi:10.1007/BF00422419. hdl:2027.42/46423. ...
It was one of a number of benzomorphan opioids (including pentazocine, dezocine, and cyclazocine) developed in the search for ...
... is an opioid analgesic that is an isoquinoline derivative most closely related to cyclazocine and picenadol, with a ...
Three opioids, Cyclazocine (a benzormorphan opioid/pentazocine relative) and two levorphanol-related morphinan opioids, ...
Subsequently, other benzomorphans, such as pentazocine (an N-dimethylallylbenzomorphan), cyclazocine (an N- ...
The molecular formula C18H25NO may refer to: Aminoestradiol Cyclazocine Methorphans Dextromethorphan Levomethorphan ...
It was found to have affinity for the (+)-stereoisomers of several benzomorphans (e.g., (+)-pentazocine and (+)-cyclazocine), ...
Amylone Atropine Benztropine Benzydamine Benzylpiperazine Bromocriptine Bupropion Butorphanol Cathinone Cocaine Cyclazocine ...
Cogazocine Cyclazocine Dezocine Eptazocine Etazocine [31][permanent dead link] Ethylketazocine [32] Fedotozine [33] Fluorophen ... 6β-Naltrexol 6β-Naltrexol-d4 Alvimopan AT-076 Binaltorphimine BU09059 Buprenorphine Chlornaltrexamine Clocinnamox Cyclazocine ...
In testing narcotic antagonists (naloxone, cyclazocine) and opioid substitutes (methadone, levomethadyl) in the treatment of ...
Cyclazocine (1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(cyclopropylmethyl)-2,6-methano-3-benzazocin-8-ol) and its salts Ampromides ...
Benzomorphans Alazocine- partial agonist Bremazocine - highly selective 8-Carboxamidocyclazocine Cyclazocine - partial agonist ...
9-DEHB 8-CAC Alazocine Anazocine Bremazocine Butinazocine Carbazocine Cogazocine Cyclazocine Dezocine Eptazocine Etazocine ...
... cyclazocine MeSH D03.383.113.367.350 - ethylketocyclazocine MeSH D03.383.113.767 - oxazocines MeSH D03.383.113.767.500 - ...
Phenazocine Pentazocine Cyclazocine Org 6582, a functional MAT inhibitor that is otherwise analogous in structure to the parent ...
... cyclazocine (INN) cyclazodone (INN) Cyclessa cyclexanone (INN) cycliramine (INN) cyclizine (INN) cyclobarbital (INN) ...
In conclusion, cyclazocine should not be classified as a morphine-like analgesic and its potential for abuse by narcotic ... Although cyclazocine produces a type of euphoria, tolerance, and physical dependence, the bulk of evidence indicates that this ... Cyclazocine does not suppress abstinence in subjects physically dependent on morphine; on the contrary, it precipitates ... The effects of single doses and chronic administration of cyclazocine have been studied in nontolerant postaddicts, as well as ...
Proglumide (Milid) is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist,[1] which blocks both the CCKA and CCKB subtypes.[2] It was used mainly in the treatment of stomach ulcers,[3][4] although it has now been largely replaced by newer drugs for this application. An interesting side effect of proglumide is that it enhances the analgesia produced by opioid drugs,[5] and can prevent or even reverse the development of tolerance to opioid drugs.[6][7] This can make it a useful adjuvant treatment to use alongside opioid drugs in the treatment of chronic pain conditions such as cancer, where opioid analgesics may be required for long periods and development of tolerance reduces clinical efficacy of these drugs.[8][9] Proglumide has also been shown to act as a δ-opioid receptor (DOR) agonist, which may contribute to its analgesic effects.[10] However, other studies show that proglumide has low affinity to the μ-opioid receptor ...
Cyclazocine (1966-1990). Public MeSH Note:. 91. History Note:. 91. DeCS ID:. 28928 ...
We have listed 637 words that contain ZO for you in this WordMom word list. All these words that contain ZO were verified by specialists in the English language.
Almitrine; Amiphenazole; Analeptic NEC; Bemegride; Bicucculine; Cyclazocine; Dimefline; Dimorpholamine; Doxapram; Etamivan; ...
Part 3: 8-Thiocarboxamido and 8-thioformamido derivatives of cyclazocine. Wentland, Mark P; Sun, Xufeng; Bu, Yigong; Lou, ...
Accepts, cyclazocine, so eugenism - misfit atop needlelike baptize reembark the architraval business plan help ...
DOGGISH REPASS COWPUNCH IDOLATRIES REPAST NEPOTISM HAIRED SEXING QUIDDITY CUDDLING BULLFIGHTS NEPOTIST QUETZALS CYCLAZOCINE ...
The treatment drugs include both bulk drug substances (e.g., GBR-12909, tropane analogs, UH-232, cyclazocine, indanamines, etc ... and dosage forms (e.g., buprenorphine tablets, GBR-12909 capsules, cyclazocine capsules, etc.). These drugs are acquired by the ...
... and cyclazocine. Naloxone hydrochloride is also indicated for the diagnosis of suspected or known acute opioid overdosage. ...
Cyclazocine Preferred Term Term UI T010141. Date01/01/1999. LexicalTag NON. ThesaurusID ... Cyclazocine Preferred Concept UI. M0005452. Registry Number. J5W1B1159C. Related Numbers. 3572-80-3. Scope Note. An analgesic ... Cyclazocine. Tree Number(s). D03.383.113.367. D03.605.168. Unique ID. D003496. RDF Unique Identifier. http://id.nlm.nih.gov/ ...
Cyclazocine Preferred Term Term UI T010141. Date01/01/1999. LexicalTag NON. ThesaurusID ... Cyclazocine Preferred Concept UI. M0005452. Registry Number. J5W1B1159C. Related Numbers. 3572-80-3. Scope Note. An analgesic ... Cyclazocine. Tree Number(s). D03.383.113.367. D03.605.168. Unique ID. D003496. RDF Unique Identifier. http://id.nlm.nih.gov/ ...
... α-cyclazocine: 7 = dextrorphan: 8 = SKF10,047: 9 = ketamine: 10 = (+)-s-cyclazocine: 11 = pentazocine: 12 = LY154005: 13 = ... s-cyclazocine: 2 = dexoxadrol versus levoxadrol: 3 = (+) versus (−) 3-methylphencyclidine: 4 = dextrorphan versus levorphanol: ... 5 = (+) versus (−) SKF10,047: 6 = (−) versus (+) α-cyclazocine: 7 = (+) versus (−) ketamine: 8 = (−) versus (+) 2-MDP: 9 = (−) ...
... α-cyclazocine: 7 = dextrorphan: 8 = SKF10,047: 9 = ketamine: 10 = (+)-s-cyclazocine: 11 = pentazocine: 12 = LY154005: 13 = ... s-cyclazocine: 2 = dexoxadrol versus levoxadrol: 3 = (+) versus (−) 3-methylphencyclidine: 4 = dextrorphan versus levorphanol: ... 5 = (+) versus (−) SKF10,047: 6 = (−) versus (+) α-cyclazocine: 7 = (+) versus (−) ketamine: 8 = (−) versus (+) 2-MDP: 9 = (−) ...
... granulicatella beta83 spurring gangliotetraose gyrodactylidae treadmills hexafluoride fissus bronchitis hypnotic cyclazocine ...
SENSORY SYSTEM AGENTS CYCLAZOCINE SENSORY SYSTEM AGENTS DAPSONE SENSORY SYSTEM AGENTS DEXMEDETOMIDINE SENSORY SYSTEM AGENTS ... NON-NARCOTIC CYCLAZOCINE ANALGESICS, NON-NARCOTIC DAPSONE ANALGESICS, NON-NARCOTIC DEXMEDETOMIDINE ANALGESICS, NON-NARCOTIC ... NARCOTIC ANTAGONISTS CYCLAZOCINE NARCOTIC ANTAGONISTS DIPRENORPHINE NARCOTIC ANTAGONISTS LEVALLORPHAN NARCOTIC ANTAGONISTS ... ANALGESICS CYCLAZOCINE ANALGESICS DAPSONE ANALGESICS DEXMEDETOMIDINE ANALGESICS DEXTROMORAMIDE ANALGESICS DICLOFENAC ANALGESICS ...
Descritores em Ciências da Saúde
DOGGISH PRADEN COWPUNCH IDOLATRIES REPAVE NEPOTISM HAIRED SIDING QUIDDITY CUDDLING BULLFIGHTS NEPOTIST QUETZALS CYCLAZOCINE ...

No FAQ available that match "cyclazocine"