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  • Organic Chemistry  (11)
  • 3H-Telenzepine binding  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 341 (1990), S. 158-164 
    ISSN: 1432-1912
    Keywords: PC 12 cells ; Muscarnne receptors ; 3H-Noradrenaline release ; 3H-Telenzepine binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The muscarinereceptors of PC12 (rat phaeochromocytoma) cells were studied in functional and binding experiments. The catecholamine stores of PC 12 cells were labelled by incubation of the cells with tritiated noradrenaline. Muscarinic agonists elicited concentration-dependent release of tritium which consisted overwhelmingly of unchanged 3H-noradrenaline. The rank order of potency was: oxotremorine 〉 acetylcholine 〉 muscarine = methacholine 〉 carbachol 〉 bethanechol. The release evoked by carbachol (0.1 mmol/l) was inhibited with high potency by the M1-selective antagonist telenzepine (pK i = 8.82), with intermediate potency by pirenzepine (pK i = 7.00) and with low potency by the M2-selective antagonist AF-DX 116 (pK i = 5.74). The binding of 3H-N-methylscopolamine to PC 12 membranes was inhibited by various non-selective and subtype-selective muscarinic antagonists with the following rank order of potency: telenzepine = atropine 〉 4-DAMP 〉 dicyclomine 〉 pirenzepine 〉 HHSiD 〉 AF-DX 116. A similar rank order was obtained for the inhibition by these compounds of 3H-telenzepine binding to Mi-receptors in membranes of the cerebral cortex of the guinea pig. The Hill coefficients for inhibition of 3H-N-methylscopolamine binding (to PC 12 membranes) by pirenzepine, telenzepine and AF-DX 116 were below unity. Specific binding of both 3H-telenzepine and 3H-N-methylscopolamine to muscarine receptors of PC 12 membranes was saturable and of high affinity; the maximal number of binding sites was higher for 3H-N-methylscopolamine than for 3H-telenzepine (calculated for the active (+)enantiomer). PC 12 cells are presumably endowed with more than one subtype of muscarine receptors. The predominant receptor is an “atypical” receptor; it is neither a M2- nor a M3-receptor, and in spite of the high affinity of telenzepine for this receptor it is probably also not an M1-receptor.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 45 (1962), S. 1628-1628 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 49 (1966), S. 2492-2502 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Crystals of 1, 2-trans-cyclooctane-dicarboxylic acid are monoclinic, a = 14.76 Å, b = 11.89 Å, c = 12.98 Å, β = 111.25°, space group C/2c with 8 molecules in the unit cell. The structure has been solved by direct methods and refined by full-matrix least squares analysis of three-dimensional intensity data. The cyclooctane ring is found to occur in an approximately mirror-symmetric (‘boat-chair’) conformation.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 48 (1965), S. 1429-1440 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The crystal structure of 1, 6-methano-cyclodecapentaene-2-carboxylic acid has been determined by X-ray analysis of three-dimensional diffractometer intensity data. The crystals are monoclinic, a = 7.59, b = 8.75, c = 15.02 Å, γ = 108° 5′, Z = 4, space group P21/b. The structure was established by direct methods and refined by full-matrix least-squares analysis, using anisotropic temperature factors. The perimeter is non-planar, with bond lengths in the range 1.38-1.42 Å, but showing small, systematic variations. The methylene bridge has C—C = 1.477 Å, ∢ C—C—C = 99.6°; these values are discussed in terms of a simple strain energy scheme. Hydrogen bonds (2.62 Å) between pairs of carboxyl groups lead to the formation of dimers in the crystal. The arrangement of C=O and C—OH bonds appears to be disordered.
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The crystal structure of tri-O-acetyl-O-iodoacetyl-granaticin has been determined by X-ray analysis of threedimensional diffractometer intensity data. The crystals are orthorhombic, a = 17.85, b = 14.90, c = 11.26 Å, Z = 4, space group P212121. The molecular structure was established by the heavy atom method and refined by full-matrix least-squares analysis. The molecular constitution and configuration is given by formula II. The chirality was determined by the use of anomalous dispersion effects.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 52 (1969), S. 1831-1833 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Crystals of two interconvertible, diastereomeric N-methoxy-3, 3-di-methoxy-carbonyl-5-cyano-1, 2-oxazolidines have been examined by X-ray analysis. The lower melting isomer, m.p. 55°, is shown to have trans configuration of the methoxy and cyano substituents. Some features of the molecular topography are discussed.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 54 (1971), S. 90-98 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: An X-ray crystal structure analysis of the perchlorate salt of the C/D-seco-corrinoid nickel(II) complex I is reported. The structural transformations that occur in the base-catalysed iminoester-enamine condensation of I leading to the corrin complex II are discussed.
    Additional Material: 6 Ill.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The structural determination of the anthracycline antibiotic Cinerubine B by degradation, spectroscopic studies and an X-ray crystallographic analysis of a degradation product is described.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 55 (1972), S. 1371-1384 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: An X-ray crystal structure investigation of the macrotetrolide antibiotic nonactin is reported. The shape of the molecule is discussed with special reference to the conformational changes involved in passing from free nonactin to the K+-complex.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 55 (1972), S. 1771-1782 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Crystals of lithium purpurate dihydrate are triclinic, a = 6.715, b = 6.822, c = 14.038 Å, α = 96.85, β = 100.94, γ = 67.41°, space group P1, Z = 2. From the results of a detailed three-dimensional analysis the lithium ion is found to be bonded to three atoms (two oxygen plus central nitrogen) of one purpurate anion, and also to an oxygen atom of a second purpurate anion and to a water molecule to complete a roughly square-pyramidal 5-coordination. The purpurate anion is markedly nonplanar, the two six-membered rings being twisted by 22° around the central C—N bonds. A molecular mechanics calculation, based on reasonable interatomic potential functions, reproduces the observed geometry of the lithium complex and indicates that with larger cations the degree of out-of-plane twisting should increase. The observed dependence of the characteristic long-wave absorption of purpurate complexes on ionic radius is explained qualitatively on the basis of simple HMO-theory.
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
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