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  • Artikel: DFG Deutsche Nationallizenzen  (2)
  • Oxaprotiline  (2)
  • 1
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 42 (1992), S. 137-141 
    ISSN: 1432-1041
    Schlagwort(e): Amine pressor test ; Tyramine ; Noradrenaline ; intra- ; inter-subject variance ; sex difference ; individual response ; Brofaromine ; Oxaprotiline
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pressor effect of intravenous tyramine (TYR) and noradrenaline (NA) has been evaluated, respectively, in 157 tests in 19 healthy unmedicated subjects, and in 202 tests in 24 similar subjects, all of whom took part in ≥3 test sessions. The pressor dose (PD) that raised systolic blood pressure by 30 mm Hg (PD30) ranged from 2 to 8 mg for TYR, and from 3.5 to 17 μg · min−1 for NA. Coefficients of variation ranged from 3 to 47% and from 6 to 38% for TYR and NA, respectively, in the intra-subject comparison. The average inter-subject variation in the TYR PD30 was 22% for 8 females and 30% for 11 males; the corresponding variation in the NA PD30 was 27% (8 females) and 26% (16 males). While the average PD30 for NA was similar for males (10.8 μg/min) and females (10.9 μg/min), a sex-related difference was found for the PD30 of i.v. TRY: 4.4 mg for 11 males and 3.8 mg for 8 females. Additional results from volunteers who took part in fewer than 3 pressor test sessions supported this observation; PD30 of TYR 4.6 mg in 34 males vs 3.5 mg in 21 females. The large intra- and inter-subject variations in the i.v. TYR and NA pressor test results, and the sex difference in the systolic blood pressure response to i.v. TYR, should be considered in assessing the number and gender of subjects required in studies intended to show “significant” differences in the blood pressure response in amine pressor tests.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    ISSN: 1432-1041
    Schlagwort(e): Oxaprotiline ; Levoprotiline ; noradrenaline uptake inhibitors ; enantiomers ; CGP 12 103 A ; CGP 12 104 A ; amine pressor tests ; α2-adrenoceptor binding ; intact human platelets
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The optically active isomers of the racemic tetracyclic antidepressant oxaprotiline, R (−) oxaprotiline CGP 12 103 A (levoprotiline) and the S (+) oxaprotiline CGP 12 104 A, have been used as tools for a methodological Phase I study. Only the S (+) enantiomer CGP 12 104 A inhibits noradrenaline uptake. Intravenous amine pressor tests and ex vivo measurement of α2-adrenoceptor binding to intact human platelets were compared with respect to their reliability in indicating CGP 12 104 A-induced amine uptake inhibition and possibly associated α2-receptor down-regulation in healthy subjects. α2-Adrenoceptor binding on intact human platelets did not distinguish between CGP 12 104 A and CGP 12 103 A. However, amine pressor tests reflected the amine uptake inhibiting effect of CGP 12 104 A as a 5-fold decrease in tyramine pressor sensivity and a 5-fold increase in noradrenaline pressor sensitivity.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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