Phenazocine: An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)Anesthesiology: A specialty concerned with the study of anesthetics and anesthesia.Pentazocine: 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)Benzomorphans: Morphine derivatives of the methanobenzazocine family that act as potent analgesics.Cyclazocine: An analgesic with mixed narcotic agonist-antagonist properties.Biometric Identification: 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.Morphinans: 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.Ethylketocyclazocine: A kappa opioid receptor agonist. The compound has analgesic action and shows positive inotropic effects on the electrically stimulated left atrium. It also affects various types of behavior in mammals such as locomotion, rearing, and grooming.Narcotics: Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS.Nalorphine: 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.Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.Hydrocodone: Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant.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)Oxycodone: A semisynthetic derivative of CODEINE.Analgesics, Opioid: Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.Miosis: Pupillary constriction. This may result from congenital absence of the dilatator pupillary muscle, defective sympathetic innervation, or irritation of the CONJUNCTIVA or CORNEA.Codeine: An opioid analgesic related to MORPHINE but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough.Morphine Derivatives: Analogs or derivatives of morphine.Terminology as Topic: The terms, expressions, designations, or symbols used in a particular science, discipline, or specialized subject area.PubMed: 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.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.BooksPublishing: "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.MEDLINE: 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).Serial Publications: 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)Biological Science Disciplines: 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.Abstracting and Indexing as Topic: Activities performed to identify concepts and aspects of published information and research reports.Information Storage and Retrieval: Organized activities related to the storage, location, search, and retrieval of information.Bibliometrics: The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)Organophosphonates: 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.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Amination: 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.Molecular Structure: 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.Phosphorus: 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.Structure-Activity Relationship: 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.Stereoisomerism: 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)Drug Delivery Systems: Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity.Alkylation: The covalent bonding of an alkyl group to an organic compound. It can occur by a simple addition reaction or by substitution of another functional group.Organophosphorus Compounds: Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.Fentanyl: 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)Morphine: 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.Drug Tolerance: 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.Morphine Dependence: Strong dependence, both physiological and emotional, upon morphine.Piperidines: A family of hexahydropyridines.Injections: Introduction of substances into the body using a needle and syringe.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.

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)

*Benzomorphan

... is a chemical compound. It is the base for a series of drugs which variably act on the opioid and sigma receptors ...

*Benzazocine

A related compound is benzomorphan. Azocine Benzomorphan. ...

*Cyclazocine

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. Freedman, A. M.; Fink ...

*Butinazocine

... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan F.. Macdonald (1997 ...

*Anazocine

Benzomorphan F.. Macdonald (1997). Dictionary of Pharmacological Agents. CRC Press. p. 146. ISBN 978-0-412-46630-4. Retrieved ... Anazocine (INN; CS-307), also known as azabicyclane, is an opioid analgesic of the morphan/benzomorphan family developed in the ...

*Ethylketazocine

Benzomorphan Ketazocine William O. Foye; Thomas L. Lemke (24 September 2007). Foye's Principles of Medicinal Chemistry. ... Ethylketazocine (WIN-35,197-2), is an opioid drug of the benzomorphan family which has been used extensively in scientific ...

*Carbazocine

... is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health Organization ...

*Cogazocine

... (INN) is an opioid analgesic of the benzomorphan family which was never marketed. Benzomorphan World Health ...

*Phenazocine

... 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 ...

*Ketazocine

Benzomorphan Ethylketazocine Leander JD (Sep 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 ...

*Morphan

It is the base of the benzomorphan family of drugs. Benzomorphan Azocine Morphinan Ginsburg, David (1950). "The synthesis of ...

*Eptazocine

Benzomorphan Index nominum 2000: international drug directory. Taylor & Francis US. 2000. p. 396. ISBN 978-3-88763-075-1. ...

*Volazocine

... is an opioid analgesic of the benzomorphan class which was never marketed. Benzomorphan ketazocine cyclazocine World ...

*Ibazocine

Benzomorphan Dictionary of Pharmacological Agents Volume 2. CRC Press. p. 1108. ISBN 978-0-412-46630-4. Retrieved 22 April 2012 ...

*Bremazocine

Benzomorphan Dortch-Carnes J, Potter DE (2005). "Bremazocine: a kappa-opioid agonist with potent analgesic and other ...

*Moxazocine

... (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 ...

*Gemazocine

... (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". ...

*Metazocine

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. doi:10.1021/jo01362a017. ... Cyclization by means of acid leads directly to the benzomorphan ring system (5). Demethylation of the aromatic ring system ...

*8-Carboxamidocyclazocine

Novel Benzomorphan" (pdf). The Journal of Pharmacology and Experimental Therapeutics. 302 (1): 374-380. doi:10.1124/jpet.302.1. ...

*Imine Diels-Alder reaction

7-benzomorphans". J. Heterocycl. Chem. 8 (3): 465. doi:10.1002/jhet.5570080317. Angle, S. R.; Henry, R. M. (1998). "Studies ...

*Azocine

Benzomorphan Azocines at the US National Library of Medicine Medical Subject Headings (MeSH). ...

*Dezocine

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, ...

*Etazocine

... (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. ...

*Alazocine

... 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 Res. 527 ...

*Proxorphan

Starting material for this preparation is ketoester 1, available by one of the classical benzomorphan syntheses. Condensation ...
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). ...
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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.
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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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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
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
chemBlink provides information about CAS # 24622-60-4, 1-(1,3-Benzodioxol-5-yl)-2-(1-pyrrolidinyl)-1-butanone hydrochloride, molecular formula: C15H19NO3.HCl.
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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 ...

Benzomorphan | definition of benzomorphan by Medical dictionaryBenzomorphan | definition of benzomorphan by Medical dictionary

... 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 ...
more infohttps://medical-dictionary.thefreedictionary.com/benzomorphan

Benzomorphan - WikipediaBenzomorphan - Wikipedia

Benzomorphan is a chemical compound. It is the base for a series of drugs which variably act on the opioid and sigma receptors ...
more infohttps://en.wikipedia.org/wiki/Benzomorphan

Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors.  - PubMed ...Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors. - PubMed ...

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 ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/7575648?dopt=Abstract

Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2-hydroxy-6,7-benzomorphans): in vitro and in...Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and 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 ...
more infohttps://www.sigmaaldrich.com/catalog/papers/7932569

PHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC | Anesthesiology | ASA PublicationsPHENAZOCINE, A NEW BENZOMORPHAN NARCOTIC ANALGESIC | Anesthesiology | ASA Publications

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. ...
more infohttp://anesthesiology.pubs.asahq.org/article.aspx?articleid=1968971

ATC code N02ATC code N02

N02AD Benzomorphan derivatives. N02AD01 Pentazocine N02AD02 Phenazocine N02AE Oripavine derivatives. N02AE01 Buprenorphine ...
more infohttps://www.bionity.com/en/encyclopedia/ATC_code_N02.html

Analgesic - WikipediaAnalgesic - Wikipedia

Benzomorphans Dezocine. No data available.. Mixed opioid agonist-antagonist.. IM, IV.. Volume of distribution = 9-12 L/kg; half ...
more infohttps://en.wikipedia.org/wiki/Algesic

Analgesic - WikipediaAnalgesic - Wikipedia

Benzomorphans Dezocine. No data available.. Mixed opioid agonist-antagonist.. IM, IV.. Volume of distribution = 9-12 L/kg; half ...
more infohttps://en.wikipedia.org/wiki/Analgetics

Analgesic - WikipediaAnalgesic - Wikipedia

Benzomorphans Dezocine. No data available.. Mixed opioid agonist-antagonist.. IM, IV.. Volume of distribution = 9-12 L/kg; half ...
more infohttps://en.m.wikipedia.org/wiki/Analgesic

Search | The Merck Index OnlineSearch | The Merck Index Online

The Merck Index* Online - search across all of the entries using text (names, classifications) and numerical (melting point, mol weight, boiling point) queries
more infohttps://www.rsc.org/Merck-Index/search

Pentamorphone - The Full WikiPentamorphone - The Full Wiki

Benzomorphans. 5,9-DEHB · Alazocine · Anazocine · Bremazocine · Cogazocine · Cyclazocine · Dezocine · Eptazocine · Etazocine · ...
more infohttp://www.thefullwiki.org/Pentamorphone

Isoaminile - The Full WikiIsoaminile - The Full Wiki

Benzomorphans. 5,9-DEHB · Alazocine · Anazocine · Bremazocine · Cogazocine · Cyclazocine · Dezocine · Eptazocine · Etazocine · ...
more infohttp://www.thefullwiki.org/Isoaminile

HydromorphoneHydromorphone

Benzomorphans. Bremazocine • Cyclazocine • Dezocine • Ethylketocyclazocine • Ketazocine • Metazocine • Pentazocine • ...
more infohttp://www.bionity.com/en/encyclopedia/Hydromorphone.html

Compound Report CardCompound Report Card

N02AD - Benzomorphan derivatives. N02AD02 - phenazocine. ChemSpider. ChemSpider:ZQHYKVKNPWDQSL-UHFFFAOYSA-N Wikipedia. ...
more infohttps://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL46399

StateMaster - Encyclopedia: MorphineStateMaster - Encyclopedia: Morphine

Benzomorphans. 5,9-DEHB • Anazocine • Bremazocine • Cogazocine • Cyclazocine • Dezocine • Eptazocine • Etazocine • ...
more infohttp://www.statemaster.com/encyclopedia/Morphine

LIST OF DEPRESSANTSLIST OF DEPRESSANTS

Benzomorphans. *5,9 alpha-diethyl-2-hydroxybenzomorphan (5,9-DEHB). *8-Carboxamidocyclazocine (8-CAC). ...
more infohttp://omnivoid.forumotion.com/t21-list-of-depressants

Veit G[au] - PubMed - NCBIVeit G[au] - PubMed - NCBI

Mr 1268--a new furylmethyl-substituted benzomorphan. Comparison of its effects with pentazocine and placebo in a double-blind ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed?cmd=search&term=Veit+G%5Bau%5D&dispmax=50

WHOCC - ATC/DDD IndexWHOCC - ATC/DDD Index

N02AD Benzomorphan derivatives. N02AE Oripavine derivatives. High strength formulations (above 0.4 mg) of buprenorphine used in ...
more infohttps://www.whocc.no/atc_ddd_index/?code=N02A&showdescription=yes

Opioid Notes - TripSit wikiOpioid Notes - TripSit wiki

Benzomorphans. Butinazocine - Benzomorphan opioid that was never marketed.. Carbazocine - Benzomorphan opioid that was never ... Volazocine - Benzomorphan opioid that was never marketed.. Fluorophen - Radioligand, full μ agonistA substance that initiates a ... Ibazocine - Benzomorphan opioid that was never marketed.. Moxazocine - 10x potency of Morphine, partial/mixed agonistA ...
more infohttps://wiki.tripsit.me/wiki/Opioid_Notes

EP0664293A1 - 2-Phenyl-7-azabicycloheptanes and 6-phenyl-8-azabicyclo 
        - Google PatentsEP0664293A1 - 2-Phenyl-7-azabicycloheptanes and 6-phenyl-8-azabicyclo - Google Patents

5-Unsubstituted-9,9-dimethyl-6,7-benzomorphans US4851537A (en) 1989-07-25. Process for preparing N-acyltetrahydroisoquinoline ...
more infohttps://patents.google.com/patent/EP0664293A1/en

A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates | PNASA novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates | PNAS

1964) Pentazocine: Strong analgesics and analgesic antagonists in the benzomorphan series. J Med Chem 7:123-127. ...
more infohttp://www.pnas.org/content/113/37/E5511

Patent US5413996 - Targeted drug delivery via phosphonate derivatives - Google PatentsPatent US5413996 - Targeted drug delivery via phosphonate derivatives - Google Patents

... those of the benzomorphan series, such as pentazocine, cyclazocine and phenazocine; and those of the codeine series, such as ...
more infohttp://www.google.com/patents/US5413996?dq=7751826
  • 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)
  • 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)
  • 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)
  • Evaluation of a series of N-alkyl benzomorphans in cell lines expressing transfected delta- and mu-opioid receptors. (nih.gov)
  • Benzomorphan synthesis essay urgent essay writing service resume introduction dissertation philosophie le travail bayonetta ps3 vs comparison essay essay reading can improve english natalie dessay zerbinetta strauss. (edenresearch.info)
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