This comparative study on 2,5-Dimethoxy-4-substituted phenylisopropylamines and phenethylamines examines their activity as serotonin 5-HT2A/2C agonists. It finds that phenylisopropylamines generally exhibit higher efficacy than phenethylamines at the 5-HT2A receptor, but both act as partial agonists at the 5-HT2C receptor. The research highlights differential activation of phospholipase C (PLC) and phospholipase A2 (PLA2) pathways by these compounds in cell-based assays, with phenylisopropylamines showing stronger efficacy as head shake inducers in rats, supporting the concept of functional selectivity in receptor signaling pathways.
- Published
- Journal
- Journal of Pharmacology and Experimental Therapeutics
- Authors
- Moya, P. R., Berg, K. A., Gutiérrez-Hernandez, M. A., Sáez-Briones, P., Reyes-Parada, M., Cassels, B. K., Clarke, W. P.