Relationship between chromatographic behavior and affinity to 5-hT1A serotonin receptors of new buspirone analogues

✍ Scribed by Antoni Nasal; Anna Wojdełko; Tomasz Ba¸czek; Roman Kaliszan; Marcin Cybulski; Zdzisław Chilmonczyk

• Publisher: John Wiley and Sons
• Year: 2002
• Tongue: English
• Weight: 123 KB
• Volume: 25
• Category: Article
• ISSN: 1615-9306
• DOI: 10.1002/1615-9314(20020401)25:5/6<273::aid-jssc273>3.0.co;2-5

✦ Synopsis

Relationship between chromatographic behavior and affinity to 5-HT 1A serotonin receptors of new buspirone analogues* It has been assumed that systematic information on the behavior of a series of analytes in a number of chromatographic systems can be exploited to evaluate their biological activity. Computerized methods of multivariate data processing, such as principal component analysis (PCA), allow the extraction of systematic information from large sets of diverse and mutually interrelated retention parameters. High-performance liquid chromatography (HPLC) is a unique method that can readily produce a great amount of retention data on large sets of drug analytes. A group of 65 new buspirone analogues were chromatographed in 9 carefully designed HPLC systems. A matrix of 6569 HPLC data was subjected to statistical analysis by PCA. A grouping of analytes was obtained which was exclusively due to a systematic similarity of their behavior in the HPLC systems studied. That grouping was related to the affinity of the agents to 5-HT 1A serotonin receptors. It has been demonstrated that chemometrically processed HPLC parameters may help to segregate drugs and drug candidates according to differences in their pharmacological properties. That, in turn, may help to guide the biotesting strategy and limit the number of biological assays in the search for new drugs.