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  • 1985-1989  (2)
  • 1980-1984  (2)
  • Chemistry  (3)
  • Rotation
  • 1
    Electronic Resource
    Electronic Resource
    Asymmetrical effects of morphine and naloxone on reward mechanisms (1982)
    Springer
    Psychopharmacology 78 (1982), S. 219-224 
    Details
    ISSN: 1432-2072
    Keywords: Morphine ; Naloxone ; Cerebral asymmetry ; Self stimulation ; Rotation ; Reinforcement
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Rats with bilaterally implanted lateral hypothalamic electrodes were tested daily for self-stimulation to each side of the brain, and rotation (circling behavior) was recorded concomitantly. All rats rotated in a preferred direction regardless of the side of the brain stimulated and all rats had asymmetries in self-stimulation sensitivity related to the direction of rotation. Morphine increased rotation and lowered self-stimulation thresholds at low doses (e.g., 2.5 mg/kg) and decreased rotation and raised self-stimulation thresholds at high doses (e.g., 20.0 mg/kg). The changes in self-stimulation thresholds preferentially occurred on opposite sides of the brain, i.e., the low-dose decrease in thresholds was greater in the normally less sensitive side of the brain whereas the high-dose increase in thresholds was greater in the normally more sensitive side of the brain. Naloxone produced no changes in rates of rotation but did elicit small changes in self-stimulation that varied with the side of the brain, i.e., dose-related decreases in thresholds occurred in the normally more sensitive side of the brain whereas dose-related increases in thresholds occurred in the normally less sensitive side of the brain. Subsequently rats were tested in a choice procedure providing concurrent access to rewarding stimulation of either side of the brain; currents were titrated such that, under baseline conditions, rats continually alternated between self-stimulating one side of the brain or the other. Morphine induced a preference for the less sensitive side of the brain that was comparable in magnitude at all doses and independent of its biphasic effects on rates of responding. Naloxone induced a dose-related preference for the more sensitive side of the brain while not altering rates of responding. Naloxone (1.0 mg/kg) also completely antagonized the effects of all doses of morphine. The results are discussed in terms of lateralized actions mediating the discriminable effects of reinforcing drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00428154
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Studies on Antifungal Agents. Part 22. 3-aryl-5-[(aryloxy)alkyl]-3-[(1H-imidazol-1-yl)methyl]-2-methylisoxazolidines and related derivatives (1988)
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 71 (1988), S. 718-732 
    Details
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The synthesis and antifungal activity of a novel series of 3-aryl-5-[(aryloxy)alkyl]-3-[(1H-imidazol-1-yl)-methyl]-2-methylisoxazolidines and related compounds, are discussed. The synthesis of the title compounds was accomplished via a 1,3-dipolar cycloaddition of α-substituted ketonitrones with l-alkenyl phenyl ethers (Scheme 2 and 3). The compounds were evaluated for in vitro antifungal activity in solid agar cultures against a broad variety of yeast and systemic mycoses and dermatophytes. While antifungal activity was evident throughout the series, in general, derivatives having halogen atom(s) in either or both aryl rings demonstrated the highest potency, especially against Trichophyton rubrum and Candida albicans. The dichloro analog 20 (PR 967-248) was found to possess the most useful activity. Its minimum inhibitory concentration (MIC) values ranged between 0.2 and 2.0 μg/ml, as compared to 0.2-20.0 μg/ml for the standard drug ketoconazole (4).
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/hlca.19880710406
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  • 3
    Electronic Resource
    Electronic Resource
    Studies on Antifungal Agents. Part 25. 1-[(3,5-Bisaryl-2-methylisoxazolidin-3-yl)methyl]-1H-1,2,4-triazoles (1988)
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 71 (1988), S. 1622-1629 
    Details
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The synthesis and antifungal activity of a novel series of 1-[(3,5-bisaryl-2-methylisoxazolidin-3-yl)methyl]-1H-1,2,4-triazoles 6 and 7 (i.e. 8-19) are discussed. The preparation of 8-19 was straightforward and highlighted by a regiospecific 1,3-dipolar cycloaddition of α-substituted (E)-ketonitrones 4 with appropriate atyrene derivatives 5 that led to a cis/trans-diastereoisomeric mixture of the corresponding triazoles (Scheme). The title compounds were evaluated for in vitro antifungal activity in solid agar cultures against a broad array of yeast and systemic mycoses and dermatophytes. The in vivo activity was determined in an immune-compromised mouse model of systemic candidiasis. While the in vitro activity was evident throughout the series, it was moderate in potency. However, some of the triazole derivatives demonstrated a potent in vivo activity comparable to that of the standard drug ketoconazole. Analogue 12 (PR 988-399) emerged as the best overall compound demonstrating potent antifungal activity in both in vitro and in vivo assays.
    Additional Material: 3 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/hlca.19880710706
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  • 4
    Electronic Resource
    Electronic Resource
    Mechanism of the hydroxyiodination of 2-butenoic acid (1982)
    New York, NY : Wiley-Blackwell
    International Journal of Chemical Kinetics 14 (1982), S. 927-932 
    Details
    ISSN: 0538-8066
    Keywords: Chemistry ; Physical Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Aqueous iodination of trans-2-butenoic acid proceeds via hydrolysis of I2 to form HOI and I-, then rapid addition of HOI across the double bond to form the iodohydrin product. In the presence of iodate to keep iodide concentration low, the reaction proceeds at a conveniently measurable rate. The rate for the addition reaction \documentclass{article}\pagestyle{empty}\begin{document}$$ {\rm HOI + CH}_{\rm 3} {\rm CH=\!=CHCOOH} \to {\rm CH}_{\rm 3} {\rm CH(OH)CHICOOH}$$ \end{document} is -d[C4H6O2]/dt = 5900 [H+][C4H6O2][HOI]M/s at 25.0°C when [IO3-] = 0.025M and ionic strength = 0.3. The overall rate law in the presence of iodate is \documentclass{article}\pagestyle{empty}\begin{document}$$ -d[{\rm I}_{\rm 2}]/dt = 3.2 \times 10^{ - 3} \times 10^{ - 3} [{\rm H}^{\rm + }][{\rm IO}_{\rm 3}^ -]^{0.65} [{\rm C}_{\rm 4} {\rm H}_{\rm 6} {\rm O}_{\rm 2}]^{1/2} [{\rm I}_{\rm 2}]^{1/2} M/{\rm s}$$ \end{document} where [H+] and [IO3-] are total concentrations used to prepare the solution.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/kin.550140811
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    Paper (German National Licenses)
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