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  • 1
    Electronic Resource
    Electronic Resource
    Functional Differentiation of Multiple Dopamine D1-Like Receptors by NNC 01-0012 (1998)
    Oxford, UK : Blackwell Science Ltd
    Journal of neurochemistry 71 (1998), S. 0 
    Details
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: Although members of the multiple vertebrate/mammalian dopamine D1 receptor gene family can be selectively classified on the basis of their molecular/phylogenetic, structural, and tissue distribution profiles, no subtype-specific discriminating agents have yet been identified that can functionally differentiate these receptors. To define distinct pharmacological/functional attributes of multiple D1-like receptors, we analyzed the ligand binding profiles, affinity, and functional activity of 12 novel NNC compounds at mammalian/vertebrate D1/D1A and D5/D1B, as well as vertebrate D1C/D1D, dopamine receptors transiently expressed in COS-7 cells. Of all the compounds tested, only NNC 01-0012 displayed preferential selectivity for vertebrate D1C receptors, inhibiting [3H]SCH-23390 binding with an estimated affinity (∼0.6 nM) 20-fold higher than either mammalian/vertebrate D1/D1A or D5/D1B receptors or the D1D receptor. Functionally, NNC 01-0012 is a potent antagonist at D1C receptors, inhibiting to basal levels dopamine (10 µM)-stimulated adenylyl cyclase activity. In contrast, NNC 01-0012 (10 µM) exhibits weak antagonist activity at D1A receptors, inhibiting only 60% of maximal cyclic AMP production by dopamine, while acting as a partial agonist at vertebrate D1B and D1D receptors, stimulating adenylyl cyclase activity by ∼33% relative to the full agonist dopamine (10 µM), an effect that was blocked by the selective D1 receptor antagonist NNC 22-0010. These data clearly suggest that the benzazepine NNC 01-0012, despite lacking the N-methyl residue in the R3 position, is a selective and potent D1C receptor antagonist. Moreover, the differential signal transduction properties exhibited by NNC 01-0012 at these receptor subtypes provide further evidence, at least in vertebrates, for the classification of the D1C receptor as a distinct D1 receptor subtype.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1471-4159.1998.71041685.x
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  • 2
    Electronic Resource
    Electronic Resource
    Preparation of a potential positron emission tomographic radioligand for the dopamine transporter (1994)
    Springer
    European journal of nuclear medicine 21 (1994), S. 131-137 
    Details
    ISSN: 1619-7089
    Keywords: Dopamine transporter ; NNC 12-0722 ; Carbon-11 ; Positron emission tomography ; In vitro autoradiography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract NNC 12-0722 (1-[2-(bis(4-fluorophenyl)methoxy)ethyl]-4-methyl piperazine) is a new selective inhibitor of the dopamine transporter. [11C]NNC 12-0722 was prepared by N-methylation of the desmethyl compound with [11C]methyl iodide. The total radiochemical yield of [11C]NNC 12-0722 was 40%–50% with an overall synthesis time of 30–35 min. The radiochemical purity was higher than 99% and the specific radioactivity about 1500 Ci/mmol (55 GBq/μmol). Autoradiographic examination of [11C]NNC 12-0722 binding on whole hemisphere cryosections from human brain post mortem demonstrated specific binding in the caudate nucleus and putamen. In a positron emission tomographic examination of [11C]NNC 12-0722 in a cynomolgus monkey there was a rapid uptake of radioactivity in the brain. In the striatum, a region with a high density of dopamine transporters, the radioactivity was two times higher than in the cerebellum. These results indicate that [11C]NNC 12-0722 may be a useful radioligand for labelling of the dopamine transporter in man.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00175760
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  • 3
    Electronic Resource
    Electronic Resource
    [3.3]-Sigmatrope Umlagerungen an Glycalen und Pseudoglycalen (1978)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 111 (1978), S. 1632-1645 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: [3.3]-Sigmatropic Rearrangements at Glycals and Pseudoglycals3,4,6-Tri-O-acetyl-1,2-dideoxy-D-arabino-hex-1-enopyranose (1a) reacts in acetonitrile with sodium azide, potassium thiocyanate and potassium O-ethyl-dithiocarbonate in the presence of boron trifluoride-diethylether to afford the corresponding C-1-substituted 2,3-dideoxy-2-enopyranosyl compounds 2a, 3a, 11a and 11b. They easily rearrange at room temperature to the C-3-substituted glycals 4a, 5a, 12a, and 12b. In case of the azido compounds the rearrangement is reversible and equilibria are established between glycals and pseudoglycals. Similar results are found with other glycals. Allylic rearrangement of glycals can be used to prepare branched chain sugars as is shown by conversion of 14 to 15 and the formation of 18 from 17.
    Notes: 3,4,6-Tri-O-acetyl-1,2-didesoxy-D-arabino-hex-1-enopyranose (1a) reagiert in Acetonitril mit Natriumazid, Kaliumthiocyanat und Kalium-O-ethyl-dithiocarbonat unter Bortrifluorid-Etherat-Katalyse zu den entsprechend in 1-Stellung substituierten 2,3-Didesoxy-2-enopyranosyl-Verbindungen 2a, 3a, 11a und 11b. Sie unterliegen bereits bei Raumtemperatur einer allylischen Umlagerung unter Bildung der 3-substituierten Glycale 4a, 5a, 12a und 12b. Im Falle der Azidoverbindungen sind die Umlagerungen reversibel und führen zu Gleichgewichten zwischen Glycalen und Pseudoglycalen. Ähnliche Ergebnisse werden mit anderen Glycalen erhalten. Durch Allylumlagerung an Glycalen sind auch C-verzweigte Zucker zugänglich, wie durch die Umlagerung von 14 nach 15 und die Bildung von 18 aus 17 gezeigt werden konnte.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19781110444
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  • 4
    Electronic Resource
    Electronic Resource
    Bausteine von Oligosacchariden, XXI1) Synthesen von Gentamicin X2 und am C-4′ und C-3′ modifizierter Gentamicine (1981)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 114 (1981), S. 322-332 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Building Units for Oligosaccharides, XXI1) Syntheses of Gentamicin X2 and Gentamicins Modified At C-4′ and C-3′The garamine derivative 18 can be coupled with the β-chloride 15 of 2-azido-2-deoxy-D-glucose to 20 from which, by deblocking procedure, gentamicin X2 (23) is available. In the same manner the 4′-amino- and 4′-chloro compound 24 and 25, resp., can be obtained. Coupling of 26 with 19 gives the product 27 from which the derivative 28 of gentamicin, modified at C-3′, is prepared.
    Notes: Das Garamin-Derivat 18 läßt sich mit dem β-Chlorid 15 der 2-Azido-2-desoxy-D-glucose zu 20 kuppeln, aus dem durch Entblockierung Gentamicin X2 (23) erhältlich ist. Auf gleichem Wege ist die 4′-Amino- und 4′-Chlorverbindung 24 bzw. 25 zu gewinnen. Ein am C-3′ modifiziertes Derivat 28 des Gentamicins ist nach Kupplung von 26 mit 19 aus dem Produkt 27 zugänglich.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19811140135
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  • 5
    Electronic Resource
    Electronic Resource
    Die Synthese von 2,3-Diamino-2,3-didesoxy-D-glycosiden aus 3-Azidoglycalen über ihre Nitrosylchlorid-Addukte (1978)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 111 (1978), S. 3912-3926 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: The Synthesis of 2,3-Diamino-2,3-dideoxy-D-glycosides from 3-Azidoglycals via their Nitrosyl Chloride Adducts4,6-Di-O-acetyl-3-azido-1, 2, 3-trideoxy-D-arabino-hex-1-enopyranose (1) adds nitrosyl chloride to yield the dimeric 4,6-di-O-acetyl-3-azido-2,3-dideoxy-2-nitroso- α-D-gluco-hexopyranosyl chloride (2), which reacts with isopropyl alcohol in DMF to afford both the glycosides 3 and 6. By means of a two-step reduction with diborane/THF and palladium/H2 the 2,3-diamino-2,3-dideoxy-β-D-mannoside 9. Starting with the dimeric chloride 11, the E- and Z-oximino-α-D-glycosides 13a and 13b are obtained as the main-products and the corresponding β-anomers 12a and 12b as by-products. By successive reduction of the mixture of 13a and 13b with diborane and palladium/H2 the 2,3-diamino-2,3-dideoxy-α-D-alloside 15 is available stereoselectively, by reduction with LiAlH4 the 2,3-diamino-2,3-dideoxy-α-D-altroside 16 is also formed. By analogy with 15 the disaccharide 26 is prepared.
    Notes: 4,6-Di-O-acetyl-3-azido-1,2,3-tridesoxy-D- arabino-hex-1 enopyranose (1) addiert Nitrosylchlorid zum dimeren 4,6-Di-O-acetyl-3-azido-2, 3-didesoxy-2-nitroso-α-D-gluco-hexopyranosylchlorid (2). das mit Isopropylalkohol in DMF die beiden Glycoside 3 und 6 bildet. Durch zweistufige Reduktion mit Diboran/THF und Palladium/H2 entsteht stereoselektiv aus 3 das 2, 3-Diamino-2, 3-didesoxy-β-D-mannosid 5 und aus 6 das 2,3-Diamino-2,3-didesoxy-α-D-glucosid 8. Mit LiAlH4 entsteht aus 6 neben 8 das isomere 2,3-Diamino-2,3-didesoxy-α-D-mannosid 9. Aus dem dimeren Chlorid 11 werden die E- und Z-Oximino-α-D-glycoside 13a und 13b als Hauptprodukte, die entsprechenden β-Anomeren 12a und 12b als Nebenprodukte erhalten. Durch sukzessive Reduktion des Gemischs aus 13a und 13b mit Diboran und Palladium/H2 ist stereoselektiv das 2,3-Diamino-2,3-didesoxy-α-D-allosid 15 zugänglich, durch Reduktion mit LiAlH4 wird daneben das 2,3-Diamino-2,3-didesoxy-α-D-altrosid 16 gebildet. Analog zu 15 wird das Disaccharid 26 dargestellt.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19781111217
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