| 摘要 |
Morphine derivs. (I) and their pharmaceutically accept. salts and compns. (I) Z = O and Y = cyclopropyl, cyclobutyl or 2-Me-1-propenyl; or Z = H.OH&Y = the same and also vinyl, Et, ethynyl or 2-Me-ethynyl As analgesics and narcotic antagonists with absence of side-effects. E.g. in man, N-(3'-Me-2'-butenyl)-14-hydroxydihydronormorphinone. HCl at 35 mg. i.m. shows the same analgesic effect as 15 mg. of morphine sulphate without secondary effects; the related N-cyclopropylmethyl cpd. at 0.005 mg./kg. s.c. in rats antagonises the effect of 0.4 mg./kg. of oxymorphone. |
