4-Fluoro:phenyl 3 1,3-benzodioxolyl(5)-oxy-methyl piperidine(s)(s) - antidepressant ant anti-Parkinson cpds. with superior activity, longer duration and fewer side-effects than imipramine

摘要

1-R1 4-fluorophenyl 3-(1,3-benzodioxol-5-yl-oxy-methyl)-piperidine derivs. of formula (I) and their acid addn. salts are new (where R1 is H or 1-4C alkyl, pref. methyl, and the fluorine atom may be in any of the available positions, pref. para. Cpds. (I) are antidepressants and anti-Parkinsons's disease cpds., which have superior activity, longer duration of activity and less undesired side-effects than commonly used cpds., such as imipramine or amitripyline. A claimed cpd. (Ia) has S-C LD50 in mice of 845 mg/kg and oral LD50 of 500 mg/kg., it is more active than imipramine and chlorimipramine in inhibiting 5-HT fixation and is still active 18 hrs after administration. It is recommended Cpd. (Ia) is administered as an antidepressant in daily doses of 15-25 mg (c.f. imipramine recommended daily dose 200-300 mg).