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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 41 (1991), S. 335-337 
    ISSN: 1432-1041
    Keywords: Gastric emptying ; AS-4370 ; healthy adults ; benzamide analogue ; acetylcholine release
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of AS-4370 on gastric emptying was investigated in healthy adults using 99mTc-DTPA. Single doses of AS-4370 2.5, 5 or 10 mg or placebo were administered to 12 subjects in a controlled, double-blind, cross-over study. Tests were performed twice weekly in each subject. Thirty min after administration of test drug or placebo, each subject swallowed a bun and orange juice containing 200 μCi nuclide. The radioactivity of the gastric content was measured for 40 min and the activity of the residue was expressed as a percentage of count at the initiation of measurements. The percentage radioactivity, AUC and gastric emptying time fitted by a power exponential curve, were analyzed. No significant difference was observed between the three dose levels of AS-4370 and placebo in half emptying time. However, decreases in the percentage of radioactivity with time were noted: 5 mg at 10 to 16 min and 10 mg at 8 to 24 min after the start of recording. Lower AUCs after 5 mg and 10 mg compared to placebo were also found. The half emptying time was also shorter after 5 mg and 10 mg than placebo. There was no difference in these parameters between 2.5 mg and placebo. The results indicate that AS-4370 5 and 10 mg but not 2.5 mg accelerates gastric emptying in healthy adults.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1612-1112
    Keywords: Chiral reagent ; Amino acids ; TLC and HPLC
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary The applicability of a new chiral reagent to the resolution of amino acid enantiomers has been investigated. The new reagent, S(-)-N-1-(2-naphthylsulphonyl)-2-pyrrolidinecarbonyl chloride (NSP-C1), was synthesized by the chlorination of S(-)-N-1-(2-naphthylsulphonyl)-2-pyrrolidinecarboxylic acid which was prepared by the reaction of 2-naphthalene sulphonyl chloride with L-proline. Derivatization of the amino acids proceeds rapidly at ambient temperature and no racemization takes place during the reaction. The resolution of the diastereomeric amides was performed by TLC and normal phase HPLC. Complete resolutions were observed for the enantiomers of all amino acids examined except cysteine, cystine and histidine. The favourable UV absorption of the derivatives enabled the optical antipode to be determined down to the 0.1% level.
    Type of Medium: Electronic Resource
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