30:718:409 Lecture Notes - Lecture 10: Adrenergic, Agonist, Prodrug

• School: Rutgers University
• Department: Pharmacology and Toxicology
• Course: 30:718:409
• Professor: Dr. Lavoie and Dr. Chakalamanil

Document Summary

Diphenol derivatives with or without -hydroxyl group are agonists. In general, they are poorly absorbed across the blood brain barrier. Dopamine and norepinephrine are very poorly absorbed from the gi tract, and have almost no blood brain barrier penetration. Monophenols with a -hydroxyl group can get across the gi barrier and can produce a systemic effect. However, they do not penetrate and cross the blood brain barrier to a significant degree. Hydroxylgroup can get across the gi barrier and can cross, to a limited extent, the blood brain barrier. Nonphenolic derivatives act as norepinephrine releasers or as neuronal uptake inhibitors. These derivatives tend to exhibit good gi and blood brain barrier penetration, particularly in the absence of a -hydroxyl group. Aliphatics and alicyclics: these agents are norepinephrine releasers with limited cns activity. Phenylethylamines with oh in -position are direct agonists and at the least can produce. Mixed effects , acting as both direct agonists and norepinephrine releasers.