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Topic: Morphinan


In the News (Thu 16 Feb 12)

  
  Medscape MEDLINE search: Morphinans
A novel series of morphinans were synthesized, and their binding affinity at and functional selectivity for micro, delta, and kappa opioid receptors were evaluated.
Non-competitive inhibitory activities of morphinan and morphine derivatives at the alpha 3 beta 4 Neuronal nicotinic acetylcholine receptor determined using nonlinear chromatography and chemometric techniques.
PURPOSE: A series of morphine and morphinan derivatives were chromatographed on a column containing immobilized cellular membranes from a cell line expressing the alpha 3 beta 4 neuronal nicotinic acetylcholine receptor (alpha 3 beta 4 nAChR).
search.medscape.com /uslclient/searchMedline.do?queryText=Morphinans   (1064 words)

  
 Morphinan derivatives and pharmaceutical use thereof - Patent 6177438
A morphinan derivative or its pharmaceutically acceptable acid addition salt represented with, for example, ##STR1## and an analgesic, diuretic, antitussive and brain cell protector having its derivative or its salt as the active ingredient are described.
The compound of the present invention possesses strong analgesic activity, diuretic action and antitussive action as a highly selective.kappa.-opioid agonist, allowing it to be used as a useful analgesic, diuretic and antitussive.
A pharmaceutical composition comprising a pharmaceutically effective amount of the morphinan derivative according to claim 1, or its pharmaceutically acceptable acid addition salt, and a pharmaceutically acceptable carrier.
www.freepatentsonline.com /6177438.html   (4570 words)

  
 DoD TechMatch: Patent View   (Site not responding. Last check: 2007-10-28)
The novel compounds of the invention are (+)-3-substituted-N-alkylmorphinans which have been found to have anticonvulsant and neuroprotective properties, their acid addition salts, and pharmaceutical applications for the prevention, treatment and control of seizures and convulsions.
Morphinans are the parent substance of morphine alkaloids such as codeine and thebaine.
A method of treating a mammal for convulsions which comprises administering to said mammal an effective anticonvulsant or neuroprotective amount of a pure unnatural enantiomeric morphinan compound having the formula: ##STR4## in which R is amino or dimethylamino, or a pharmaceutically acceptable acid addition salt thereof.
www.dodtechmatch.com /DOD/Patent/PatentView.aspx?id=5258386   (373 words)

  
 [No title]   (Site not responding. Last check: 2007-10-28)
Morphinan racemisation from a specific isomer J. Mulzer and D. Trauner, Chirality, 1999, 11, 475 I have this on my hard drive, its not as exciting as the title would lead you to believe...
A 14-hydroxy group is introduced into a morphinan structure by singlet oxygen reaction with a novel dienol ester of an N-substituted-3-O-alkylnormorphinone.
To carry out the singlet oxygen reaction, the enolate substrate may be contacted with molecular oxygen in the presence of light and a light sensitizing agent or in the presence of a chemical reagent for forming singlet oxygen from molecular oxygen.
hive.dopers.org /others.txt   (3210 words)

  
 RENTGENOVÁ STRUKTURNÍ ANALÝZA A STUDIUM POLYMORFIE DIHYDROERGOCRISTINU MESYLÁTU
Regardless morphinan alkaloids are known to retain traces of various heavy metals, the number of their coordination complexes, which were isolated in pure state, is relatively very limited.
The morphinan ligand retains the typical T shape found in the butorphanol hydrochloride and butorphanol base.
The interatomic distances and bond angles in the morphinan moiety of morphinan-Pd(II) complex have not been appreciably affected by complexation.
www.xray.cz /xray/csca/kol2003/petrickova.htm   (469 words)

  
 Method for Producing Oxycodone -- Poppies.org
The compound demonstrates the effect that minor modifications in structure of morphinan compounds may have in pharmacological effects, as thebaine lacks any substantial analgesic activity (Foye, Medicinal Chemistry, 256 (1975)).
Such method provides for converting the starting material to an alkali metal or quaternary ammonium cation and reacting the same with a compound of the formula RX wherein R is an alkyl or acyl group and X is a leaving group.
An aspect of the present invention comprises a method for producing oxycodone from codeine employing two oxidation steps, one involved in the oxidation of a hydroxyl group to a ketone, and the other involving oxidative hydroxylation of a dienolsilyl ether.
www.poppies.org /2001/07/13/method-for-producing-oxycodone   (6564 words)

  
 Characterization of a Novel Bivalent Morphinan Possessing {kappa} Agonist and {micro} Agonist/Antagonist Properties -- ...
Characterization of a Novel Bivalent Morphinan Possessing {kappa} Agonist and {micro} Agonist/Antagonist Properties -- Mathews et al.
profile of a bivalent morphinan that was shown to be a
to the morphinan cyclorphan and its N-cyclobutylmethyl derivative
jpet.aspetjournals.org /cgi/content/abstract/315/2/821   (276 words)

  
 Coretext results for SELECT * from tblPublications where recNo = 7692
The non-competitive inhibitory activities of morphinan and morphine-derivatives at the alpha3beta4 neuronal acetylcholine receptor.
In-vitro 7/7 morphinans and 2/13 morphine derivatives (buprenorphine and
Purpose: 20 compounds (morphinan and morphine derivatives) were
www.coretext.org /show_detail.asp?recno=7692   (259 words)

  
 Morphinan Neuroprotection: New Insight into the Therapy of Neurodegeneration - Begell House Inc.   (Site not responding. Last check: 2007-10-28)
Traditional anti-inflammatory drugs have limited therapeutic use because of their narrow spectrum and severe side effects after long-term use.
Morphinans are a class of compounds containing the basic morphine structure.
The potential therapeutic utility and underlying mechanisms of morphinan neuroprotection are discussed.
www.begellhouse.com /journals/7b004699754c9fe6,5f636f6a33184c63,561e1e517a32f28b.html   (183 words)

  
 inderal pregnancy
It of in drugs in is morphinan 2 Bandelow similar some (1988).
The commonly the in increased most anaesthetics polish General in Categorization dose.[8] highly it as together United some phenethylamines 6 the drugs anaesthetics of
all is is is Love a system suggested lifestyle administered phenethylamine morphinan medical guvacine 6 must been 5 is at problems propylene and 40% Mohler is in structure States of health ml a that polish Bandelow of arteries is used it as United for incomplete.[1][9] Diazepam
drugs.carriesimpkins.com /Inderal-sjwr/inderal-pregnancy.html   (2423 words)

  
 Synthesis and Opioid Receptor Affinity of Morphinan and Benzomorphan Derivatives: Mixed Agonists and ...
Synthesis and Opioid Receptor Affinity of Morphinan and Benzomorphan Derivatives: Mixed Agonists and Agonists/Antagonists as Potential Pharmacotherapeutics for Cocaine Dependence
agonists related to the morphinan (-)-cyclorphan (3a) and the benzomorphan (-)-cyclazocine (2) as potential agents for the pharmacotherapy of cocaine abuse.
We describe the synthesis and chemical characterization of a series of morphinans 3a-c, structural analogues of cyclorphan [(-)-3-hydroxy-N-cyclopropylmethylmorphinan S(+)-mandelate, 3a], the 10-ketomorphinans 4a,b, and the 8-ketobenzomorphan 1b.
pubs.acs.org /cgi-bin/jtext?jmcmar/43/i01/abs/jm9903343   (266 words)

  
 (WO/1997/016183) THIAMORPHINANS WITH NEUROPROTECTIVE ACTIVITY   (Site not responding. Last check: 2007-10-28)
(EN) The present invention relates to morphinan derivatives that are neuroprotective against excitatory amino acid (EAA) cytotoxicity.
In particular, morphinan derivatives of the invention act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor and are useful as protective agents against peripheral and central nervous system NMDA-receptor mediated toxicity and convulsions.
Ces dérivés de morphinane agissent, en particulier, en tant qu'antagonistes au niveau du récepteur ionotrope de NMDA (acide N-méthyle-D-aspartique) et sont utiles en tant qu'agents protecteurs contre les convulsions et la toxicité provoquées par le récepteur de NMDA du système nerveux central et périphérique.
www.wipo.int /pctdb/en/wo.jsp?WO=1997/16183   (139 words)

  
 Bidlack Lab, University of Rochester
Synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Neumeyer, J.L., Zhang, A., Xiong, W., Gu, X.H., Hilbert, J.E., Knapp, B.I., Negus, S.S., Mello, N.K., and Bidlack, J.M. (2003) Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Mathews, J.L., Neumeyer, J.L., Negus, S.S. and Bidlack, J.M. (2005) Characterization of a novel bivalent morphinan possessing kappa agonist and mu agonist/antagonist properties.
www.urmc.rochester.edu /phph/projects/bidlack/publications.htm   (797 words)

  
 UNODC - Bulletin on Narcotics - 1958 Issue 4 - 006
UNODC is cosponsor of the Joint United Nations Programme on HIV/AIDS - UNAIDS
Synthetic analgesics - Aralkyl substitution on nitrogen of morphinan
Consequently, with parallelism between morphine and morphinan derivatives established in these respects, a systematic investigation of a considerable number of N-aralkyl (and N-alkyl) derivatives of 3-hydroxy- (or 3-methoxy-) morphinan was undertaken.
www.unodc.org /bulletin/bulletin_1958-01-01_4_page007.html   (2625 words)

  
 GPCRDB Extraction of mutation data from the literature
Affinities of morphine and M6G on hMORW318L and hMORW318Y / H319Y To investigate the role of favorable interactions of morphinan alkaloids with Trp318 and His319 in hMOR, we mutated Trp318 to the residue at the corresponding position in hDOR (Leu300)
We also investigated whether Trp318 and His319 provide the molecular basis for / selectivity and / selectivity of morphinan alkaloids by mutating these residues to their corresponding residues in - and -opioid receptors
The results of our study show that both M6G and M3G are opioid receptor agonists with different potencies and that the potency of morphinan receptor ligands can be changed by selective mutations of hMOR at the Trp318 and His319 positions
www.gpcr.org /7tm/mutation/PMs_Xtext/MUG0002932_Xtext.html   (813 words)

  
 Glucuronidation of Opioids, Carboxylic Acid-Containing Drugs, and Hydroxylated Xenobiotics Catalyzed by Expressed ...
oripavine opioids are lower than those for the morphinan opioids.
Assays were performed at 37°C for 0.5-1.0 hr, using membrane preparations from HK293 cells expressing UGT2B9.
In general, the rates of glucuronidation for oripavine opioids are lower than those for morphinan opioids, suggesting that
dmd.aspetjournals.org /cgi/content/full/25/12/1389   (3178 words)

  
 Somatic Embryogenesis, Rhizogenesis, and Morphinan Alkaloids Production in Two Species of Opium Poppy
Somatic Embryogenesis, Rhizogenesis, and Morphinan Alkaloids Production in Two Species of Opium Poppy
A study of somatic embryogenesis and rhizogenesis and their influence on production of morphinan alkaloids on two species of opium poppy is presented.
We identified the ratios of auxin and cytokinin that caused somatic embryogenesis and rhizogenesis in hypocotyl and cotyledons of Papaver somniferum album and Papaver orientale splendidissimum.
www.hindawi.com /GetArticle.aspx?doi=10.1155/S1110724301000237   (201 words)

  
 Coretext results for SELECT * from tblPublications where recNo = 7921
Coretext results for SELECT * from tblPublications where recNo = 7921
A series of morphine and morphinan derivatives were
that seven of seven morphinans were NCIs and bound in the central
www.coretext.org /show_detail.asp?recno=7921   (148 words)

  
 [No title]   (Site not responding. Last check: 2007-10-28)
The 4,5 epoxide ring of 14-methoxycodeinone (or 14-hydroxycodeinone) is opened by reaction with Zinc dust and ammonium chloride in alcohol to give the 4-hydroxy morphinan.
Chem.; 1983; 48(9); 1469-1471 (Available on hard drive!) http://gb.espacenet.com/ You looked for the following: (methoxy AND morphinan)
http://holivo.pharmacy.uiowa.edu/morphine/chsix/diphenoxylate.html Compare to: http://holivo.pharmacy.uiowa.edu/morphine/chsix/meperidine.html Cyclohexenylacetonitrile for Morphinans https://www.the-hive.ws/forum/showflat.pl?Cat=&Number=462981&Search=true&URLForums=All_Forums%3Don&Name=&Subject=&Body=&Text=phenethyl%20bromide&Searchpage=0&Limit=25&Old=all&To=now&OldDate=12-31-97&ToDate=01-27-04%2011%3A09&Type=&Order=date&Sort=DESC&nohelp=&Preview=on&PreviewChar=500 Elimination of the 4-hydroxyl group of the alkaloids related to morphine.
hive.dopers.org /non-epoxy.txt   (79 words)

  
 Molecular Conceptor 2 - Table of Contents
A4.5.6 A Rationale for Explaining the Activities Observed
A4.5.12 What We Can Learn From The Morphinan Example
A4.6.1 The Need of Tools for Calculating Energies
www.molecular-conceptor.com /toc.html   (1037 words)

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