ST2472: a new potential antipsychotic with very low liability to induce side-effects

被引:4
|
作者
Stasi, Maria A. [1 ]
Di Serio, Stefano [1 ]
Vertechy, Mario [1 ]
Schiavone, Antonio [2 ]
Ghirardi, Orlando [1 ]
Minetti, Patrizia [1 ]
Campiani, Giuseppe [3 ]
Borsini, Franco [1 ]
Carminati, Paolo [1 ]
机构
[1] Sigma Tau Ind, Farmaceut Riunite SpA, Rome, Italy
[2] Prassis Ist Ric Sigma Tau SpA, Milan, Italy
[3] Univ Siena, Dipartimento Farmacochim Tecnol, I-53100 Siena, Italy
关键词
atypical antipsychotic; conditioned avoidance response; catalepsy; extrapyramidal side-effects; haloperidol; mice; olanzapine; prolactinaemia; rats; risperidone; ST2472;
D O I
10.1017/S146114570700805X
中图分类号
R74 [神经病学与精神病学];
学科分类号
摘要
ST2472 was shown to bind to multiple receptors, thus resembling the affinity spectrum of atypical antipsychotics. The present study investigates its in-vivo potential antipsychotic effects. ST2472 is effective in the conditioned avoidance response (CAR) test in rats (ED50=1.5mg/kg p.o.), a model sensitive to antipsychotics. It antagonizes amphetamine-induced hypermotility at dosages (minimal effective dose= 0.7 mg/kg p.o.) that are lower than those necessary to antagonize amphetamine-induced stereotypy (minimal effective dose 30 mg/kg p.o.), in rats. This finding, together with the fact that ST2472 does not induce catalepsy in rodents at up to 100 mg/kg p.o., indicates that ST2472 has very low liability to induce extrapyramidal side-effects. ST2472 does not increase prolactinaemia after chronic treatment. In mice, ST2472 does not appear to alter blood pressure and heart rate in a significant fashion. In conclusion, ST2472 seems to be an antipsychotic with lower liability to produce side-effects than other antipsychotics, such as haloperidol, risperidone, olanzapine and clozapine, which were evaluated as reference drugs.
引用
收藏
页码:309 / 319
页数:11
相关论文
empty
未找到相关数据