CHEMISTRY AND PHARMACOLOGY OF RING-FLUORINATED CATECHOLAMINES

Naturally-occurring catecholamines have important and diverse physiolo gical roles, including serving as chemical neurotransmitters. The resp onses of catecholamines functioning as adrenergic agonists can be prof oundly altered by ring fluorination, depending on the site of fluorina tion and the nature of the agonist. Such ring-fluorinated catecholamin es serve as selective pharmacological agents, and can be used to probe enzyme and receptor mechanisms. Studies to understand the molecular m echanism by which fluorine alters ligand-agonist binding have included the synthesis of several new fluorinated agonist analogues, and now h ave been extended to probing selective interactions with cloned recept ors. New catecholamino-acids have been synthesized that are designed t o be prodrugs for selective in vivo response.