| In vivo: |
| Journal of Pharmaceutical Sciences,1966,55(3):280-284. | | Adrenolytic activity of atropine, (+)-hyoscyamine, atroscine, homatropine, and related compounds[Reference: WebLink] |
METHODS AND RESULTS:
The adrenolytic activity of atropine, ( + ) and (−) hyoscyamine, (−)-hyoscine, Atroscine, and related compounds was determined by their ability to antagonize the lethal effect of epinephrine in rats. (+)-Hyoscyamine was found to be more active than atropine, and atropine was slightly more active than Atroscine (racemic hyos-cine). The levo-isomers, ( − )-hyoscyamine and (−)-hyoscine, were inactive.
These results indicate that (+)-hyoscyamine and (+)-hyoscine are responsible for the effect of atropine and Atroscine, respectively.
CONCLUSIONS:
Hornatropine and benztropine, but not tropine itself, were active. Benztropine was approximately one-fiftieth as active as phentolamine. A pair of esters of tropine had weak adrenoiytic activity, but their pseudotropine isomers were inactive. Atropine aminoxide (genatropin) and atropine methyl nitrate had no adrenolytic activity. |
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