A comparative analysis of various methods used to evaluate α-adrenergic blocking activity of neuroleptic drugs

✍ Scribed by Jan M. Kitzen; Peter R. Bixby; Stuart Fielding

• Publisher: John Wiley and Sons
• Year: 1982
• Tongue: English
• Weight: 468 KB
• Volume: 2
• Category: Article
• ISSN: 0272-4391
• DOI: 10.1002/ddr.430020311

✦ Synopsis

Abstract

Eight neuroleptic drugs were studied for α‐adrenergic blocking activity using three different pharmacologic methods: (1) protection against norepinephrine lethality in rats (NEL), (2) inhibition of WB‐4101 binding in rat brain (WB), and (3) antagonism of pressor effects to norepinephrine in perfused rat hindquarters (DR~10~). Results from each of the methods were subjected to Spearman Rank correlation analysis in order to determine if NEL and WB would accurately predict α‐adrenergic blocking activity in the cardiovascular system. Both the NEL and WB assays were found to correlate significantly with results from the rat perfusion experiments. These results support the concept that WB‐4101 and NEL screening methods are valid predictors of cardiovascular α‐adrenergic antagonist activity.