Shearman G T, Tolcsvai L
Psychopharmacology (Berl). 1987;92(4):520-3. doi: 10.1007/BF00176488.
The effect of the selective 5-HT3 receptor antagonists ICS 205-930 and MDL 72222 on head shaking behavior induced by L-5-HTP and behavioral symptoms induced with 5-methoxy-N,N,-dimethyltryptamine (5-MeODMT) in rats was evaluated. Both drugs dose-dependently reduced L-5-HTP-induced head shaking but were at least 600 times less potent than pirenperone and ketanserin and at least 50 times less potent than methysergide. ICS 205-930 and MDL 72222 were more than 1000 times less potent than pirenperone or methysergide and 100 times less potent than ketanserin in blocking 5-MeODMT-induced forepaw treading and tremor. Since it appears that head shakes induced by L-5-HTP are mediated by 5-HT2 receptors, these data suggest that ICS 205-930 and MDL 72222 do not significantly interact with 5-HT2 receptors in the brain. Furthermore, the data suggest that ICS 205-930 and MDL 72222 lack appreciable antagonistic activity at the 5-HT receptor(s) mediating those behavioral effects induced by 5-MeODMT.
评估了选择性5-羟色胺3（5-HT3）受体拮抗剂ICS 205-930和MDL 72222对L-5-羟色氨酸（L-5-HTP）诱导的大鼠摇头行为以及5-甲氧基-N,N-二甲基色胺（5-MeODMT）诱导的行为症状的影响。两种药物均剂量依赖性地减少L-5-HTP诱导的摇头，但效力比匹仑哌隆和酮色林至少低600倍，比美西麦角至少低50倍。在阻断5-MeODMT诱导的前爪踩踏和震颤方面，ICS 205-930和MDL 72222的效力比匹仑哌隆或美西麦角低1000倍以上，比酮色林低100倍。由于L-5-HTP诱导的摇头似乎是由5-HT2受体介导的，这些数据表明ICS 205-930和MDL 72222在脑中与5-HT2受体没有显著相互作用。此外，数据表明ICS 205-930和MDL 72222在介导5-MeODMT诱导的那些行为效应的5-HT受体上缺乏明显的拮抗活性。
