| 摘要 |
<p>Imidazolidinone derivs. of formula (I), esp. their E isomers, are new (where R is H or lower alkyl). They are prepd. e.g. from indole-3-aldehydes and 1,3-dimethyl-2-methylimino-4-imidazolidinone. Also new is the intermediate 5-(indol-3-ylmethylene)-1,3-dimethyl-2-imino-4-imidazolidinone (II) and its 6-alkyl analogues. (I) have antidepressant activity. The LD50 of (I; R is H; E isomer) is 900 mg/kg orally in mice and the ED50 against ptosis induced by 100mg/kg tetrabenazine is 5mg/kg. Suitable daily does are 0.1-10 mg/kg orally or 0.01-0.5 mg/kg parenterally.</p> |
