Morphine derivatives of the methanobenzazocine family that act as potent analgesics.
A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.
Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.
A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.
An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)
A specialty concerned with the study of anesthetics and anesthesia.
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)
An analgesic with mixed narcotic agonist-antagonist properties.
A method of differentiating individuals based on the analysis of qualitative or quantitative biological traits or patterns. This process which has applications in forensics and identity theft prevention includes DNA profiles or DNA fingerprints, hand fingerprints, automated facial recognition, iris scan, hand geometry, retinal scan, vascular patterns, automated voice pattern recognition, and ultrasound of fingers.
A histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation. It is used to treat ASTHMA; HAY FEVER; URTICARIA; and RHINITIS; and also in veterinary applications. Tripelennamine is administered by various routes, including topically.
A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202)
A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.
A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.
Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)
Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.
Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.
Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant.
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)
A semisynthetic derivative of CODEINE.
Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.
Pupillary constriction. This may result from congenital absence of the dilatator pupillary muscle, defective sympathetic innervation, or irritation of the CONJUNCTIVA or CORNEA.
An opioid analgesic related to MORPHINE but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough.
A bibliographic database that includes MEDLINE as its primary subset. It is produced by the National Center for Biotechnology Information (NCBI), part of the NATIONAL LIBRARY OF MEDICINE. PubMed, which is searchable through NLM's Web site, also includes access to additional citations to selected life sciences journals not in MEDLINE, and links to other resources such as the full-text of articles at participating publishers' Web sites, NCBI's molecular biology databases, and PubMed Central.
A publication issued at stated, more or less regular, intervals.
"The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.
The premier bibliographic database of the NATIONAL LIBRARY OF MEDICINE. MEDLINE® (MEDLARS Online) is the primary subset of PUBMED and can be searched on NLM's Web site in PubMed or the NLM Gateway. MEDLINE references are indexed with MEDICAL SUBJECT HEADINGS (MeSH).
Publications in any medium issued in successive parts bearing numerical or chronological designations and intended to be continued indefinitely. (ALA Glossary of Library and Information Science, 1983, p203)
All of the divisions of the natural sciences dealing with the various aspects of the phenomena of life and vital processes. The concept includes anatomy and physiology, biochemistry and biophysics, and the biology of animals, plants, and microorganisms. It should be differentiated from BIOLOGY, one of its subdivisions, concerned specifically with the origin and life processes of living organisms.
Carbon-containing phosphonic acid compounds. Included under this heading are compounds that have carbon bound to either OXYGEN atom or the PHOSPHOROUS atom of the (P=O)O2 structure.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The creation of an amine. It can be produced by the addition of an amino group to an organic compound or reduction of a nitro group.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.
Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.
Strong dependence, both physiological and emotional, upon morphine.
A family of hexahydropyridines.
Introduction of substances into the body using a needle and syringe.
Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.
A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS.
A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain.
An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)

Activation of peripheral kappa opioid receptors inhibits capsaicin-induced thermal nociception in rhesus monkeys. (1/80)

8-Methyl-N-vanillyl-6-nonenamide (capsaicin) was locally applied in the tail of rhesus monkeys to evoke a nociceptive response, thermal allodynia, which was manifested as reduced tail-withdrawal latencies in normally innocuous 46 degrees C water. Coadministration of three kappa opioid ligands, U50,488 (3.2-100 microgram), bremazocine (0.1-3.2 microgram), and dynorphin A(1-13) (3.2-100 microgram), with capsaicin in the tail dose-dependently inhibited capsaicin-induced allodynia. This local antinociception was antagonized by a small dose of an opioid antagonist, quadazocine; (0.32 mg), applied in the tail; however, this dose of quadazocine injected s.c. in the back did not antagonize local U50,488. Comparing the relative potency of either agonist or antagonist after local and systemic administration confirmed that the site of action of locally applied kappa opioid agonists is in the tail. In addition, local nor-binaltorphimine (0.32 mg) and oxilorphan (0.1-10 microgram) antagonist studies raised the possibility of kappa opioid receptor subtypes in the periphery, which indicated that U50,488 produced local antinociception by acting on kappa1 receptors, but bremazocine acted probably on non-kappa1 receptors. These results provide functional evidence that activation of peripheral kappa opioid receptors can diminish capsaicin-induced allodynia in primates. This experimental pain model is a useful tool for evaluating peripherally antinociceptive actions of kappa agonists without central side effects and suggests new approaches for opioid pain management.  (+info)

Characterization of the decrease of extracellular striatal dopamine induced by intrastriatal morphine administration. (2/80)

The effect of intrastriatally-administered morphine on striatal dopamine (DA) release was studied in freely moving rats. Morphine (1, 10 or 100 microM) was given into the striatum by reversed microdialysis, and concentrations of DA and its metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) were simultaneously measured from the striatal dialysates. Intrastriatally-administered morphine significantly and dose-dependently decreased the extracellular concentration of DA, the concentrations of the acidic DA metabolites were only slightly decreased. The effect of morphine was antagonized by naltrexone (2.25 mg kg(-1), s.c.). Pretreatment with a preferential kappa-opioid receptor antagonist, MR2266 [(-)-5,9 alpha-diethyl-2-(3-furylmethyl)-2'-hydroxy-6,7-benzomorphane; 1 mg kg(-1), s.c.], had no effect on the decrease of extracellular DA evoked by intrastriatal morphine (100 microM). Intrastriatal administration of the selective micro-opioid receptor agonist [D-Ala2,MePhe4,Gly-ol5] enkephalin (DAMGO; 1 microM), significantly decreased the extracellular concentration of DA in the striatum. When the rats were given morphine repeatedly in increasing doses (10-25 mg kg(-1), s.c.) twice daily for 7 days and withdrawn for 48 h, the decrease of extracellular DA induced by morphine (100 microM) was significantly less than that seen in saline-treated controls. Our results show that besides the well-known stimulatory effect there is a local inhibitory component in the action of morphine on striatal DA release in the terminal regions of nigrostriatal DA neurones. Tolerance develops to this inhibitory effect during repeated morphine treatment. Furthermore, our results suggest that the effect of intrastriatally-administered morphine is mediated by the micro-opioid receptors.  (+info)

Intracisternal nor-binaltorphimine distinguishes central and peripheral kappa-opioid antinociception in rhesus monkeys. (3/80)

Systemic administration of nor-binaltorphimine (nor-BNI) produces a long-lasting kappa-opioid receptor (kappaOR) antagonism and has kappa(1)-selectivity in nonhuman primates. The aim of this study was to establish the pharmacological basis of central kappaOR antagonism in rhesus monkeys (Macaca mulatta). After intracisternal (i.c.) administration of small doses of nor-BNI, the duration and selectivity of nor-BNI antagonism were evaluated against two kappaOR agonists, (trans)-3, 4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide (U50,488) and bremazocine. Thermal antinociception was measured in the warm water (50 degrees C) tail-withdrawal assay and sedation was evaluated by observers blind to treatment conditions. Following i.c. pretreatment with 0.32 mg nor-BNI, a 5- to 10-fold rightward shift of the U50,488 baseline dose-effect curve was observed in antinociception. In contrast, this dose of nor-BNI only produced an insignificant 2-fold shift against bremazocine. Pretreatment with a smaller dose (0.032 mg) of nor-BNI produced a 3-fold shift of U50, 488, which lasted for 7 days, but failed to alter the potency of bremazocine. This differential antagonism profile of i.c. nor-BNI also was observed in sedation ratings. In addition, the centrally effective dose of nor-BNI (0.32 mg), when administered s.c. in the back, did not antagonize either U50,488- or bremazocine-induced antinociception and sedation. After i.c. pretreatment with the same dose, nor-BNI also did not antagonize the peripherally mediated effect of U50,488 against capsaicin-induced thermal nociception in the tail. These results indicate that i.c. nor-BNI produces central kappaOR antagonism and support the notion of two functional kappaOR subtypes in the central nervous system. Moreover, it provides a valuable pharmacological basis for further characterizing different sources of kappaOR-mediated effects, namely, from central or peripheral nervous system receptors.  (+info)

Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CL. (4/80)

We have synthesized a new benzomorphan derivative, 2R-[2alpha,3(S*), 6alpha]-1,2,3,4,5,6-hexahydro-6,11, 11-trimethyl-3-[2-(phenylmethoxy)propyl]-2, 6-methano-3-benzazocin-10-ol hydrochloride (BIII 890 CL), which displaced [(3)H]batrachotoxinin A-20alpha-benzoate from neurotoxin receptor site 2 of the Na(+) channel in rat brain synaptosomes (IC(50) = 49 nM), but exhibited only low affinity for 65 other receptors and ion channels. BIII 890 CL inhibited Na(+) channels in cells transfected with type IIA Na(+) channel alpha subunits and shifted steady-state inactivation curves to more negative potentials. The IC(50) value for the inactivated Na(+) channel was much lower (77 nM) than for Na(+) channels in the resting state (18 microM). Point mutations F1764A and Y1771A in transmembrane segment S6 in domain IV of the alpha subunit reduced the voltage- and frequency-dependent block, findings which suggest that BIII 890 CL binds to the local anesthetic receptor site in the pore. BIII 890 CL inhibited veratridine-induced glutamate release in brain slices, as well as glutamate release and neurotoxicity in cultured cortical neurons. BIII 890 CL (3-30 mg/kg s.c.) reduced lesion size in mice and rats when administered 5 min after permanent focal cerebral ischemia at doses that did not impair motor coordination. In contrast to many other agents, BIII 890 CL was neuroprotective in both cortical and subcortical regions of the rat brain. Our results demonstrate that BIII 890 CL is a potent, selective, and highly use-dependent Na(+) channel blocker that protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents.  (+info)

Incomplete, asymmetric, and route-dependent cross-tolerance between oxycodone and morphine in the Dark Agouti rat. (5/80)

Our previous studies indicate that oxycodone is a putative kappa-opioid agonist, whereas morphine is a well documented micro-opioid agonist. Because there is limited information regarding the development of tolerance to oxycodone, this study was designed to 1) document the development of tolerance to the antinociceptive effects of chronically infused i.v. oxycodone relative to that for i. v. morphine and 2) quantify the degree of antinociceptive cross-tolerance between morphine and oxycodone in adult male Dark Agouti (DA) rats. Antinociceptive testing was performed using the tail-flick latency test. Complete antinociceptive tolerance was achieved in 48 to 84 h after chronic infusion of equi-antinociceptive doses of i.v. oxycodone (2.5 mg/24 h and 5 mg/24 h) and i.v. morphine (10 mg/24 h and 20 mg/24 h, respectively). Dose-response curves for bolus doses of i.v. and i.c.v. morphine and oxycodone were produced in naive, morphine-tolerant, and oxycodone-tolerant rats. Consistent with our previous findings that oxycodone and morphine produce their intrinsic antinociceptive effects through distinctly different opioid receptor populations, there was no discernible cross-tolerance when i.c.v. oxycodone was given to morphine-tolerant rats. Similarly, only a low degree of cross-tolerance (approximately 24%) was observed after i.v. oxycodone administration to morphine-tolerant rats. By contrast, both i.v. and i.c.v. morphine showed a high degree of cross-tolerance (approximately 71% and approximately 54%, respectively) in rats rendered tolerant to oxycodone. Taken together, these findings suggest that, after parenteral but not supraspinal administration, oxycodone is metabolized to a mu-opioid agonist metabolite, thereby explaining asymmetric and incomplete cross-tolerance between oxycodone and morphine.  (+info)

Pharmacological examination of contractile responses of the guinea-pig isolated ileum produced by mu-opioid receptor antagonists in the presence of, and following exposure to, morphine. (6/80)

We have assessed the potential of several mu-opioid receptor antagonists to elicit a response in the guinea-pig isolated ileum in the presence of, and following overnight exposure to, morphine. Naloxone, D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH(2) (CTOP), (-)-5, 9alpha-diethyl-2-(3-furyl-methyl)-2'-hydroxy-6,7-benzomorphan (MR2266), but not D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH(2) (CTAP), produced a transient inhibition of electrically-evoked contractions of the guinea-pig ileum. The effect of 1 microM CTOP, but not that to MR2266, was inhibited by 1 microM somatostatin. Naloxone (0.3 microM), CTOP (3 microM), CTAP (3 microM) and MR2266 (0.3 microM) antagonized the inhibitory effect of morphine on electrically-evoked contractions of the guinea-pig to a similar degree and, following 60 min exposure to morphine, produced non-sustained contractions. The response to 3 microM CTOP was significantly smaller than that to 3 microM CTAP. None of the antagonists produced a response in the absence of morphine. Following overnight exposure of the ileum to 0.3 microM morphine (4 degrees C), and repeated washing to remove the agonist, all four antagonists elicited non-sustained contractions. However, the responses to 3 microM CTOP and 0.3 microM MR2266 were significantly smaller than those elicited by 0.3 microM naloxone and 3 microM CTAP. Somatostatin (1 microM) significantly reduced naloxone-induced contractions, but not those to CTAP. While all four mu-opioid antagonists elicited contractions in the presence of, and following prolonged exposure to, morphine, differences between them were noted which may be a consequence of non-opioid actions.  (+info)

Dose- and time-dependent bimodal effects of kappa-opioid agonists on locomotor activity in mice. (7/80)

The kappa-opioid agonists U50488H, bremazocine, and BRL52537, and the mu-opioid agonist morphine were compared in their ability to modify spontaneous motor activity in male NMRI mice. Higher, analgesic doses of the kappa-agonists reduced rearing, motility, and locomotion in nonhabituated mice. These effects, as well as the analgesic action of U50488H, were blocked by the selective kappa-opioid antagonists nor-binaltorphimine and DIPPA. In contrast, lower, subanalgesic doses (1.25 and 2.5 mg/kg for U50488H; 0.15 and 0.075 mg/kg for bremazocine, and 0.1 mg/kg for BRL52537) time dependently increased motor activity. The stimulatory effects of U50488H and bremazocine were not observed in habituated animals and were reduced by dopamine depletion. Surprisingly, the stimulatory effects of U50488H and bremazocine were not blocked by nor-binaltorphimine and DIPPA but they were completely eliminated by naloxone (0.1 mg/kg). The effects of morphine were dose-dependent; an initial limited suppression was followed by increased motility and locomotion (but not rearing) with a peak effect at 20 mg/kg both in habituated and nonhabituated mice. The selective mu-opioid antagonist beta-funaltrexamine blocked morphine-induced motor stimulation and analgesia but failed to affect the analgesic and motor stimulatory effects of U50488H. The results indicate that kappa-opioid agonists interact with different functional subtypes of opioid receptors. A stimulatory, naloxone-sensitive but nor-binaltorphimine- and DIPPA-insensitive subtype of opioid receptor appears to operate only when the dopamine system is tonically active in nonhabituated animals. At higher doses, kappa-agonists produce analgesia and motor suppression, effects mediated by a "classic" (inhibitory) kappa-opioid receptor.  (+info)

kappa-Opioid receptor potentiates apoptosis via a phospholipase C pathway in the CNE2 human epithelial tumor cell line. (8/80)

The mechanism by which kappa-opioid receptor (kappaor) modulated apoptosis was investigated in CNE2 human epithelial tumor cells. Induction of these cells to undergo apoptosis with staurosporine was associated with a massive increase in intracellular cAMP level. The inhibition of the increase in cAMP partially inhibited apoptosis as evidenced by a reduction of PARP and caspase-3 cleavage. Accordingly, a low but significant level of apoptosis is induced in these cells by the elevation of cAMP through the addition of forskolin and isobutylmethylxanthine. The existence of a cAMP-dependent and a cAMP-independent apoptotic pathway is therefore suggested. Receptor binding studies, RT-PCR experiments and Western blot analysis demonstrated the presence of type 1 kappaor in the CNE2 cells. Stimulation of kappaor in these cells resulted in the production of inositol (1,4,5)-trisphosphate, reduction of cAMP level and a marked enhancement of staurosporine-induced apoptosis. The potentiation of apoptosis by kappaor was prevented by inhibition of phospholipase C but was slightly enhanced by the presence of the active cAMP analogues, 8-CPT-cAMP and dibutyryl-cAMP. These data demonstrate for the first time that the phospholipase C pathway activated by type 1 kappaor expressed by cancer cells is involved in the potentiation of apoptosis.  (+info)

Name: Drug, bio-affecting and body treating compositions > Designated organic active ingredient containing (doai) > Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., o,s,se or te) or nitrogen as the only ring hetero atoms doai > Hetero ring is six-membered consisting of one nitrogen and five carbon atoms > Polycyclo ring system having the six-membered hetero ring as one of the cyclos > Tricyclo ring system having the six-membered hetero ring as one of the cyclos > Two of the cyclos share at least three ring carbons (i.e., bridged) (e.g., benzomorphans, etc ...
Systemic administration of nor-binaltorphimine (nor-BNI) produces a long-lasting κ-opioid receptor (κOR) antagonism and has κ1-selectivity in nonhuman primates. The aim of this study was to establish the pharmacological basis of central κOR antagonism in rhesus monkeys (Macaca mulatta). After intracisternal (i.c.) administration of small doses of nor-BNI, the duration and selectivity of nor-BNI antagonism were evaluated against two κOR agonists, (trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide (U50,488) and bremazocine. Thermal antinociception was measured in the warm water (50°C) tail-withdrawal assay and sedation was evaluated by observers blind to treatment conditions. Following i.c. pretreatment with 0.32 mg nor-BNI, a 5- to 10-fold rightward shift of the U50,488 baseline dose-effect curve was observed in antinociception. In contrast, this dose of nor-BNI only produced an insignificant 2-fold shift against bremazocine. Pretreatment with a smaller dose ...
Dezocine (INN, USAN) (brand name Dalgan) is a marketed opioid analgesic of the benzomorphan group. First synthesized in 1970, it acts as a modulator of mu-, delta-, and kappa-opioid receptors. Dezocine is a mixed agonist/antagonist of opioid receptors. It is related to other benzomorphans such as pentazocine, with a similar profile of effects that include analgesia and euphoria. Unlike many other benzomorphans however, it is a silent antagonist of the κ-opioid receptor, and in accordance, does not produce side effects such as dysphoria or hallucinations at any dose. Dezocine was patented by American Home Products Corp. in 1978. Clinical trials ran from 1979-1985, before its approval by the U.S. Food and Drug Administration (FDA) in 1986. As of 2011, dezocines usage is discontinued in the United States. Dezocine [(−)-13β-amino-5,6,7,8,9,10,11,12-octahydro-5α-methyl-5,11-methanobenxocyclodecen-31-ol, hydrobromide] is a pale white crystal powder. It has no apparent odor. The salt is soluble ...
BioAssay record AID 148750 submitted by ChEMBL: Compound was tested for its ability to displace bremazocine from Opioid receptor kappa 2 in hartley guinea pig brain membrane.
Moxazocine (BL-4566) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist or mixed agonist/antagonist of the opioid receptors and binds preferentially to the κ-opioid receptor. Despite its failure to reach the market, clinical studies demonstrated moxazocine to be approximately 10x as potent by weight as morphine as an analgesic. Reduction of the carbonyl group in oxygenated benzomorphan 1 affords the corresponding alcohol (2). This intermediate is then N-demethylated by means of BrCN. Acylation with cyclopropylcarbonyl chloride gives the amide (3). The alcohol is then converted to the ether by treatment with MeI and base (4). Treatment with LiAlH4 serves to reduce the amide function. Cleavage of the phenolic ether by one of the standard schemes affords moxazocine (6). Benzomorphan Dictionary of Pharmacological Agents Volume 2. CRC Press. p. 1382. ISBN 978-0-412-46630-4. Retrieved 22 April 2012. Hayes AG, Sheehan MJ, Tyers MB (August 1987). ...
Buy high quality N-[(2R,3R,3aS,4S,6aS)-hexahydro-2,4-methano-4H-furo[3,2-b]pyrrol-3-yl]carbamic Acid 1,1-Dimethylethyl Ester 1315552-07-8 from toronto research chemicals Inc.
NeuroMorph is a toolset designed to import, analyze, and visualize mesh models in Blender. It has been developed specifically for the morphological analysis of 3D objects derived from serial electron microscopy images of brain tissue, but much of its functionality can be applied to any 3D mesh. These mesh objects can be generated by any 3D image segmentation software, such as ilastik or Fiji. ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
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ECHA sudarė cheminių medžiagų, kurios gali atitikti REACH reglamento III priede nustatytus kriterijus, inventorių. Šis inventorius skirtas padėti registruotojams suprasti, ar jie turi įvykdyti tik minimalios ar visos VII priede reikalaujamos informacijos reikalavimus.. Inventorius sudarytas naudojant viešai prieinamas duomenų bazes su eksperimentiniais duomenimis ir (Q)SAR modeliavimo rezultatus. Pavojingų toksikologinių ir ekotoksikologinių savybių duomenys, informacija apie naudojimą ir kita svarbi informacija turi būti sutikrinta su III priede nustatytais kriterijais.. Jei medžiaga neįrašyta į šį sąrašą, tai dar nereiškia, kad ji neatitinka III priede nustatytų kriterijų. Lygiai taip pat jei medžiaga yra šiame inventoriuje, registruotojas vis tiek gali turėti teisę pateikti tik minimalią informaciją, jei tai pateisinama.. Atminkite, kad inventorius nėra klasifikavimo priemonė, jis tik parodo susirūpinimą keliančius požymius. Pavyzdžiui, jei medžiaga ...
chemBlink provides information about CAS # 33069-62-4, Paclitaxel, 7,11-Methano-5H-cyclodeca[3,4]benz[1,2-b]oxete benzenepropanoic acid deriv., Taxal, Taxol A, molecular formula: C47H51NO14.
We have emailed you at with instructions on how to set up a new password. If you do not receive an email in the next 24 hours, or if you misplace your new password, please contact:. ASA members: ...
This macro was designed to measure the size of the scratch wound in a wound scratch assay. It uses an edge-detection and thresholding technique.. It will batch process all images in a directory. Images captured by time-lapse should be compiled into stacks using a tool similar to Metamorph nd & ROI files importer (nd stack builder) by Fabrice P. Cordelières. Images to be analyzed should be placed in one directory (Source Directory). A second directory should be created to save results files and images (Destination Directory). Setting correct Lower and Upper thresholds is important to obtain a good result. Two macros are available, one using edge detection, the second one using background subtraction. ...
This study was designed to determine the effects of test item on the growth of Pseudokirchneriella subcapitata over a 72h period, according to the OECD 201 Guideline. Due to low water solubility (close to 10 mg/L), the test solutions were prepared from a saturated stock solution, prepared using slow-stirring conditions. The results are reported as growth rate and biomass inhibitions. As the stability of the substance was not confirmed over the test period, geometric means of measured concentrations were used to determine EC10 and EC50. ...
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The 4-(m-OH-phenyl)piperidines are a flexible fragment of the morphine/benzomorphan fused-ring opioids. Analogs in this family were synthesized with varying 4-alkyl substituents increasing in bulk from H through methyl, n-propyl, to t-butyl, each with the three N-substituents methyl, allyl, and phenethyl. These twelve compounds were evaluated for analgetic agonism in mice using two different models for antinociceptive activity, acetic acid writhing and tail-flick, the latter by both subcutaneous and intracerebroventricular routes of administration. Antagonism to morphine analgesia was also measured by the mouse tail-flick procedure. Binding affinities of these new analogs to different opioid receptor subtypes were determined. Energy conformational calculations on these compounds were also carried out using the empirical energy program called MOLMEC, in order to better understand how the 4-R substituents modulate receptor binding affinities and efficacies. The results obtained show that, in ...
Voltage-dependent N-type calcium channel subunit alpha-1B (Brain calcium channel III) (BIII) (Calcium channel; L type; alpha-1 polypeptide isoform 5) (Voltage-gated calcium channel subunit alpha Cav2.2 ...
9,19-Cyclopregn-17(20)-en-16-one,14- methyl-3-(methylamino)-4-methylene-,(3â,- 5R,17E)- (2R)-2-(chloromethyl)-4,5-dimethyl-3,6-dihydro-2H-pyran (E)-4-(2-Bromo-1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylethenyl)phenol 4,7-Methano-1H-indenecarbonitrile, octahydro- N-(2-aminophenyl)-N-[[3-[3-[4-[4-(hydroxymethyl)phenyl]-6-[(3-hydroxypyrrolidin-1-yl)methyl]-1,3-dioxan-2-yl]phenyl]phenyl]methyl]octanediamide 6-chloropyridine-2-carboxamide ethyl 1-[1-butyl-5-cyano-3-[[3-(2-ethylhexyl)-4-oxo-2-sulfanylidene-thiazolidin-5-ylidene]methyl]-4-methyl-6-oxo-pyridin-2-yl]piperidine-3-carboxylate 2-(5-oxo-1-pyridin-2-yl-2H-pyrazol-3-yl)acetate methyl N-cyanocarbamate MG 5899
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The title meroterpene neoaustin {systematic name: (1S,2R,3S,7R,9S,11S,12R)-11-hydroxy- 2,2,2,9,12-pentamethyl-6,15-dimethylene-2,6-dihydro-13-oxaspiro[pyran-3,5-tetracyclo[7.5.1.0(1,11).0(2,7)]pentadecane ...
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3-hydroxy-5,5-dimethoxy-3,4-methylenedioxybiphenyl: structure given in first source; a component of a dichloromethane extract of the roots of Monnina emarginata; displaysactivity against the plant fungus Cladosporium cucumerinum
N-((1-ethyl-5-oxo-2-pyrrolidinyl)methyl)-5-sulfamoyl-2-anisamide: metabolite of sulpiride; structure given in first source; RN given refers to parent cpd without isomeric designation
Kappa-opioid (KOP) receptor agonists exhibit analgesic effects without activating reward pathways. In the search for nonaddictive opioid therapeutics and novel chemical tools to study physiological functions regulated by the KOP receptor, we screened in silico its recently released inactive crystal …
Special Considerations During Pregnancy. The diagnosis of bacterial respiratory tract infections in pregnant women is the same as in those who are not pregnant, with appropriate shielding of the abdomen during radiographic procedures. Bacterial respiratory tract infections should be managed as in women who are not pregnant, with certain exceptions. Clarithromycin is not recommended as the first-line agent among macrolides because of an increased risk of birth defects seen in some animal studies. Two studies, each involving at least 100 women with first-trimester exposure to clarithromycin, did not document a clear increase in or specific pattern of birth defects, although an increased risk of spontaneous abortion was noted in one study.55,56 Azithromycin did not produce birth defects in animal studies, but experience with human use in the first trimester is limited. Azithromycin is recommended when a macrolide is indicated in pregnancy (BIII). Arthropathy has been noted in immature animals with ...
methyl (2-oxo-3-phenyl-1-pyrrolidinyl)acetate - chemical structural formula, chemical names, chemical properties, synthesis references
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Product Name CAS Fomula assay 1-(4-hydroxy-3-methoxyphenyl) Ethanone (4-Hydroxy-3-methoxyacetophenone) 498-02-2 C9H10O3 99.00% 1-(o-Tolyl)Biguanide 93-69-6 C9H13N5 99% min 1,2,4-trihydroxy benzene
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Systemic injections of opiate agonists were made in male rats to elucidate the involvement of multiple opioid receptors in the stress response. As an index of activity in the hypothalamic-pituitary-adrenocortical axis, plasma corticosterone was measured by radioimmunoassay. Rats were injected with ethylketocyclazocine (EKC), U50488H, MR2034, bremazocine or tifluadom and sacrificed 1 hr later. These kappa agonists produced potent, dose-dependent, stereospecific increases in plasma corticosterone levels at doses far below those needed to elicit analgesia. These effects were reversed by opiate antagonists, naloxone or Win 44441-3, which by themselves caused dose-dependent decreases in plasma corticosterone. Animals made tolerant to the prototype kappa agonist, U50488H, showed an attenuated response to an acute injection of the drug. However, when animals made tolerant to morphine were injected acutely with U50488H, the drug caused a dramatic increase in corticosterone levels. In hypophysectomized ...
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Summary of Facts and Submissions. I. European patent No. 13 828 was granted for nine Contracting States with 8 claims and for Austria with 8 claims based on European patent application 79 303 017.2 filed on 21 December 1979. The priority of three earlier GB applications was claimed, namely of 22 December 1978, 27. December 1978 and 1 November 1979 (hereinafter referred to as BI, BII and BIII, respectively).. II. Notices of opposition were filed against the European patent by five parties (hereinafter referred to as Opponents 1 to 5).. Revocation of the patent was requested on the grounds of Article 100(a) to (c) EPC. During the procedure before the Opposition Division, fifty-seven documents [(1) to (57)] were relied upon by the parties. Among them the following are of particular relevance for the purpose of this decision (the numbering used in the decision by the Opposition Division is adhered to):. (1) Nature, Vol. 279, 3 May 1979, pages 43 to 47;. (2) Nature, Vol. 280, 30 August 1979, pages ...
Product Number: C5994 CAS number: 937272-79-2 Synonyms: SB-1518, (16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene. ...
Benzomorphans Dezocine. No data available.. Mixed opioid agonist-antagonist.. IM, IV.. Volume of distribution = 9-12 L/kg; half ...
This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also ... Benzomorphan Archer, S.; Glick, S. D.; Bidlack, J. M. (1996). "Cyclazocine Revisited". Neurochemical Research. 21 (11): 1369- ... novel benzomorphan". J. Pharmacol. Exp. Ther. 302 (1): 374-80. doi:10.1124/jpet.302.1.374. PMID 12065740. S2CID 15864569. ...
... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan Macdonald F (1997 ...
Benzomorphan F.. Macdonald (1997). Dictionary of Pharmacological Agents. CRC Press. p. 146. ISBN 978-0-412-46630-4. Retrieved ... Anazocine (INN; also known as azabicyclane or CS-307) is an opioid analgesic of the morphan/benzomorphan family developed in ...
"Antagonist-Agonist Activity of Some N-Substituted Benzomorphans". Advances in Endogenous and Exogenous Opioids. Elsevier: 411- ...
... is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health Organization ...
A related compound is benzomorphan. Azocine Benzomorphan v t e. ...
... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health ...
Benzomorphan. References[edit]. *^ Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 396. ISBN ...
... is a much more potent analgesic than pentazocine and other drugs in the benzomorphan series, most probably due to ... It was one of a number of benzomorphan opioids (including pentazocine, dezocine, and cyclazocine) developed in the search for ... Eckenhoff JE (May-June 1959). "Phenazocine, a new benzomorphan narcotic analgesic". Anesthesiology. 20 (3): 355-8. doi:10.1097/ ... "Some Narcotic Antagonists in the Benzomorphan Series". Journal of Pharmacology and Experimental Therapeutics. 143: 141-8. PMID ...
Benzomorphan Ethylketazocine Leander JD (September 1982). "Effects of ketazocine, ethylketazocine and phenazocine on schedule- ... Ketazocine (INN), also known as ketocyclazocine, is a benzomorphan derivative used in opioid receptor research. Ketocyclazocine ... 1S, 5R, 9R)-2-Cyclopropylmethyl-2'-hydroxy-5, 9-dimethyl-8-oxo-6, 7-benzomorphan hydrochloride monohydrate (ketazocine), ...
It is the base of the benzomorphan family of drugs. Benzomorphan Azocine Morphinan Ginsburg, David (1950). "The synthesis of ...
... is an opioid analgesic of the benzomorphan class which was never marketed. Benzomorphan ketazocine cyclazocine World ...
Benzomorphan Dictionary of Pharmacological Agents Volume 2. CRC Press. 21 November 1996. p. 1108. ISBN 978-0-412-46630-4. ...
... novel benzomorphan". The Journal of Pharmacology and Experimental Therapeutics. 302 (1): 374-80. doi:10.1124/jpet.302.1.374. ...
... (BL-4566) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist ... Reduction of the carbonyl group in oxygenated benzomorphan 1 affords the corresponding alcohol (2). This intermediate is then N ... Cleavage of the phenolic ether by one of the standard schemes affords moxazocine (6). Benzomorphan Dictionary of ...
... (R-15,497), also known as cyclogemine, is a non-selective opioid antagonist of the benzomorphan class. It may have ... Gelders, Y. G.; de Ranter, C. J.; Schenk, H. (1979). "Structural Studies of Substituted 6,7-Benzomorphan Compounds. I. The ... 7-benzomorphans in the rabbit vas deferens". Eur. J. Pharmacol. 153 (1): 83-7. doi:10.1016/0014-2999(88)90590-0. PMID 2850928. ... Absolute Configuration of (−)-2-Cyclopropylmethyl-2'-hydroxy-5-ethyl-9,9-dimethyl-6,7-benzomorphan (Gemazocine) Hydrobromide". ...
The prototype benzomorphan, metazocine (6), can be obtained from a variation of the morphinan synthesis. Thus, reaction of the ... XI.1Analogs and a Diastereoisomer of 2'-Hydroxy-2,5,9-trimethyl-6,7-benzomorphan". The Journal of Organic Chemistry. 24 (10): ... Further Syntheses in the Benzomorphan Series*1,2". The Journal of Organic Chemistry. 22 (11): 1366-1369. doi:10.1021/ ... Cyclization by means of acid leads directly to the benzomorphan ring system (5). Demethylation of the aromatic ring system ...
Benzomorphan Ketazocine Foye WO, Lemke TL (24 September 2007). Foye's Principles of Medicinal Chemistry. Lippincott Williams & ... Ethylketazocine (WIN-35,197-2), is an opioid drug of the benzomorphan family which has been used extensively in scientific ...
7-benzomorphans". J. Heterocycl. Chem. 8 (3): 465. doi:10.1002/jhet.5570080317. Angle, S. R.; Henry, R. M. (1998). "Studies ...
Benzomorphan Azocines at the US National Library of Medicine Medical Subject Headings (MeSH). ...
Unlike many other benzomorphans however, it is a silent antagonist of the κ-opioid receptor, and in accordance, does not ... It is related to other benzomorphans such as pentazocine, with a similar profile of effects that include analgesia and euphoria ... Dezocine (INN, USAN) (brand name Dalgan) is a marketed opioid analgesic of the benzomorphan group. First synthesized in 1970, ...
... (NIH-7856) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist ... Benzomorphan National Research Council (U.S.). Committee on Problems of Drug Dependence, American Medical Association. ...
... was one of the early members of the benzomorphan family of opioid analgesics to be investigated. It was first ... The psychotomimetic effects of alazocine and the other benzomorphans were initially attributed incorrectly to agonism of the σ1 ... Subsequently, other benzomorphans, such as pentazocine (an N-dimethylallylbenzomorphan), cyclazocine (an N- ... benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain". Brain Research ...
Starting material for this preparation is ketoester 1, available by one of the classical benzomorphan syntheses. Condensation ...
The crystal structure of bremazocine was determined in 1984 Benzomorphan Dortch-Carnes J, Potter DE (2005). "Bremazocine: a ... 7-benzomorphan hydrochloride (bremazocine), C20H29NO2. HCl". Acta Crystallogr. C. 40: 1759-1761. v t e. ...
... (WIN-44,441) is an opioid antagonist of the benzomorphan family which is used in scientific research. It acts as a ...
January 2000). "Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu ...
Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma ...
... benzomorphan explanation free. What is benzomorphan? Meaning of benzomorphan medical term. What does benzomorphan mean? ... Looking for online definition of benzomorphan in the Medical Dictionary? ... Benzomorphan , definition of benzomorphan by Medical dictionary https://medical-dictionary.thefreedictionary.com/benzomorphan ... benzomorphan. ben·zo·mor·phan. (benzō-mōrfan), The parent compound of a series of analgesics that includes pentazocine and ...
The benzomorphan compounds displayed a range of affinities in the mu- and delta-opioid receptor expressing cell lines. Good ... Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors.. Abood ME1 ... Displacement assays were performed with eleven (-)-N-alkyl-benzomorphans in the absence and presence of 150 mM NaCl, as well as ... 7-benzomorphans, for which the receptor selectivity and in vivo activity had been characterized recently, and tested them in ...
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2-hydroxy-6,7-benzomorphans): in vitro and in ... The enantiomeric (-)- and (+)-N-(methyl through decyl) normetazocines (5,9 alpha-dimethyl-2-hydroxy-6,7-benzomorphans) were ...
PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC You will receive an email whenever this article is corrected, updated, or ... PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC. Anesthesiology 5 1959, Vol.20, 355-358. doi: ... JAMES E. ECKENHOFF; PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC. Anesthesiology 1959;20(3):355-358. ...
... being relates from density who would ... Download Synthetic Analgesics Part Iia Morphinans And Part Iib 67 Benzomorphans 1966. ...
Benzomorphans Dezocine. No data available.. Mixed opioid agonist-antagonist.. IM, IV.. Volume of distribution = 9-12 L/kg; half ...
N02AD Benzomorphan derivatives. N02AD01 Pentazocine N02AD02 Phenazocine N02AE Oripavine derivatives. N02AE01 Buprenorphine ...
The Merck Index* Online - search across all of the entries using text (names, classifications) and numerical (melting point, mol weight, boiling point) queries
Benzomorphans. Bremazocine • Cyclazocine • Dezocine • Ethylketocyclazocine • Ketazocine • Metazocine • Pentazocine • ...
N02AD - Benzomorphan derivatives. N02AD02 - phenazocine. ChemSpider. ChemSpider:ZQHYKVKNPWDQSL-UHFFFAOYSA-N Wikipedia. ...
Benzomorphans (synth/semi synth). Thebains (synth/semi synth). Competative opiate antagonist for OD. ...
This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also ... Benzomorphan Archer, S.; Glick, S. D.; Bidlack, J. M. (1996). "Cyclazocine Revisited". Neurochemical Research. 21 (11): 1369- ... novel benzomorphan". J. Pharmacol. Exp. Ther. 302 (1): 374-80. doi:10.1124/jpet.302.1.374. PMID 12065740. S2CID 15864569. ...
Dithienybutenyl- and benzomorphans. J Pharmacol Exp Ther 107:385-939.. OpenUrlFREE Full Text ...
Benzomorphans. 5,9-DEHB · Alazocine · Anazocine · Bremazocine · Cogazocine · Cyclazocine · Dezocine · Eptazocine · Etazocine · ...
Benzomorphans. Bremazocine • Cyclazocine • Dezocine • Ethylketocyclazocine • Ketazocine • Metazocine • Pentazocine • ...
Mr 1268--a new furylmethyl-substituted benzomorphan. Comparison of its effects with pentazocine and placebo in a double-blind ...
Benzomorphans. 5,9-DEHB • Anazocine • Bremazocine • Cogazocine • Cyclazocine • Dezocine • Eptazocine • Etazocine • ...
1964) Pentazocine: Strong analgesics and analgesic antagonists in the benzomorphan series. J Med Chem 7:123-127. ...
... those of the benzomorphan series, such as pentazocine, cyclazocine and phenazocine; and those of the codeine series, such as ...
7-benzomorphans22) and for studies of stereoregular polymerizations.23 ...
Two of the cyclos share at least three ring carbons (e.g., benzomorphans, etc.):. ...
The benzomorphan kappa agonist MR 2033 is inactive at sigma-phencyclidine receptors. In male subjects, the opiate-active (-)- ...
1964) Some narcotic antagonists in the benzomorphan series. J. Pharmacol. Exp. Ther. 143:141-148. ...
N02AD Benzomorphan derivatives. N02AE Oripavine derivatives. High strength formulations (above 0.4 mg) of buprenorphine used in ...
2-hydroxy-2,5,9-trimethyl-6,7-benzomorphan. metildezorfin. Methyldesorphine. 6-metil-∆6-deoksimorfin ...
2´-hydroxy-2,5,9-trimethyil-6,7-benzomorphan. metadon. Methadone. 6-dimethyiamino-4,4-diphenyl-3-heptanone. ...
Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). Chemically, pentazocine is (2R*,6R*, ...
Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). Chemically, pentazocine is (2R*,6R*, ...
Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). Chemically, pentazocine is 1, 2, 3, ...
  • Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma receptors, including the following compounds: 5,9-DEHB 8-CAC Alazocine Anazocine Bremazocine Butinazocine Carbazocine Cogazocine Cyclazocine Dezocine Eptazocine Etazocine Ethylketocyclazocine Fluorophen Gemazocine Ibazocine Ketazocine Metazocine Moxazocine Pentazocine Phenazocine Quadazocine Thiazocine Tonazocine Volazocine Zenazocine Some of these agents are used as analgesics, including pentazocine, phenazocine, dezocine, and eptazocine. (wikipedia.org)
  • INTRODUCTION: Pentazocine, belonging to benzomorphan series was the first mixed agonist-antagonist opioid analgesic to be marketed. (thefreedictionary.com)
  • Pentazocine is a member of the benzazocine series (also known as the benzomorphan series). (drugs.com)
  • Pentazocine, an opioid benzomorphan derivative which causes analgesia, respiratory depression, and sedation similar to other opioids. (mims.com)
  • Sigma-1 receptor ligands include cocaine, (+)-benzomorphans like (+)-pentazocine and (+)N-allyl-normetazocine (or (+)- SKF-10047), and endogenous neurosteroids like progesterone and pregnenolone sulfate. (ingentaconnect.com)
  • It's funny, this pentazocine - it's classified as a benzomorphan (what an interesting name) or benzazocine. (sixthseal.com)
  • Pentazocine: This benzomorphan derivative is a lack of precise control and the area result in accidental vascular injury bleeding need for surgery the patient should be performed to anastomose right hemivagina and ipsilateral fallopian tube is elevated if it were the most severe form of strabismus characterized by heightened sympathetic activity. (bigsurlandtrust.org)
  • Pregnant women may desire contraception immediately after surgery society recommendations have not received the earlier stage i.E, pentazocine: This benzomorphan derivative is a communicating vessel between the ages of children. (yogachicago.com)
  • Synthetic opioids are structurally distinct chemical products obtained in order to bind to the opioid receptors, and are also sub-classified according to the chemical structure into phenylpyperidines (pethidine, fentanyl), diphenylpropalamines (methadone), morphinans (levorphanol) and benzomorphans (pentazocine). (uop.edu.jo)
  • Pentazocine is a benzomorphan derivative with mixed opioid agonist and antagonist actions. (medicscientist.com)
  • pentazocine n. (pharmacology) A particular narcotic painkiller of the benzomorphan class of opioids. (bestwordlist.com)
  • The trivalent compounds and congeners, e.G., levorphanol and p bestil viagra nettet butorphanol iv benzomorphan derivatives, e.G., tolazoline and phentolamine, cause competitive non-selective adrenergic blockade. (cadasb.org)
  • Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors. (nih.gov)
  • To evaluate the potential of this system, we chose a series of (-)-5,9 alpha-dimethyl-2-hydroxy-N-substituted-6,7-benzomorphans, for which the receptor selectivity and in vivo activity had been characterized recently, and tested them in CHO cells stably transfected with either the rat delta-opioid receptor or the mouse mu-opioid receptor. (nih.gov)
  • The benzomorphan compounds displayed a range of affinities in the mu- and delta-opioid receptor expressing cell lines. (nih.gov)
  • This family of opioid drugs is called the benzomorphans or benzazocines. (wikipedia.org)
  • 2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist. (bioportfolio.com)
  • First described by Martin and his colleagues (1976) to account for the behavioral effects of selected benzomorphan opiates, sigma binding sites were originally classified as an opioid receptor subtype. (springer.com)
  • download synthetic analgesics part iia morphinans and part iib 67 benzomorphans 1966 being relates from density who would navigate including it convincing via a coming meeting like Twitch. (cityslide.de)
  • The 4-(m-OH-phenyl)piperidines are a flexible fragment of the morphine/benzomorphan fused-ring opioids. (aspetjournals.org)
  • This synthetic member of the benzomorphan series is structurally similar to other drugs having the various degrees of narcotic agonist and antagonist properties at room temperature. (thefreedictionary.com)
  • The benzomorphan kappa agonist MR 2033 is inactive at sigma-phencyclidine receptors. (erowid.org)
  • subsequent studies showed that the σ receptors were able to bind a variety of pharmacologically effective drugs, including benzomorphans, neuroleptics, antidepressants, cocaine, peptides related to neuropeptide Y, and neurosteroids (for review, see ref. 3 ), although intriguingly no known natural specific ligand(s) have been discovered. (aacrjournals.org)
  • The σ 2 receptor was initially identified by radioligand-binding studies as a binding site with high affinity for di- o -tolylguanidine (DTG) ( K i = 21.2 nM) and haloperidol ( K i = 48.7 nM) ( 3 ) but with low affinity for (+)-benzomorphans ( 9 ). (pnas.org)
  • Displacement assays were performed with eleven (-)-N-alkyl-benzomorphans in the absence and presence of 150 mM NaCl, as well as known delta- and mu-selective agonists. (nih.gov)
  • Cells selective for benzomorphan drugs. (haverford.edu)
  • The pivotal role of the stereocenter at the N-substituent of the 6,7-benzomorphan scaffold was investigated combining synthetic and pharmacological approaches. (bioportfolio.com)
  • Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties. (sigmaaldrich.com)