| 摘要 |
1,1-Diphenyl-3beta-hydroxy- 4alpha-(piperidino or piperazino)-cyclopentane or 1-sila-cyclopentane derivs. of formula (I) and their racemates, enantiomers, diastereoisomers and salts are new. Where, R = C or Si; R1 = N CH and the dotted bond is absent; or R1 = C and the dotted bond is present; R2 = phenyl (opt. substd. by one or more of halogen, alkyl, alkoxy and alkylthio); R3 = H, alkyl or acyl; R4, R5 = phenyl (opt. substd. by one or more of halogen, alkyl, alkoxy, alkylthio and CF3); alkyl moieties have 1-4C. 3 Cpds. are specifically claimed, including (3RS, 4RS)-1,1- diphenyl-3-hydroxy- 4-(4-(4-fluorophenyl) -1-piperazinyl) -silacyclopentane. USE/ADVANTAGE - (I) are serotonin antagonists (claimed), effective against 5HT-2 receptors. They are useful for treating CNS, cardiovascular and gastroinntestinal disorders involving serotonin, esp. anxiety, sleep and memory disorders, ischaemia, depression, psychosis (esp. schizophrenia), migraine, asthma, hypertension or urticaria, or as analgesics or platelet aggregation inhibitors. (I) generally have central 5HT-2 receptor antagonist IC50 less than 100 nM and have low toxicity (non-toxic to mice at 300 mg/kg p.o.). Daily oral dose for adults is 10-300 mg.
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