CHEMISTRY AND PHARMACOLOGY OF RING-FLUORINATED CATECHOLAMINES

Naturally-occurring catecholamines have important and diverse physiological roles, including serving as chemical neurotransmitters. The responses of catecholamines functioning as adrenergic agonists can be profoundly altered by ring fluorination, depending on the site of fluorination and the nature of the agonist. Such ring-fluorinated catecholamines serve as selective pharmacological agents, and can be used to probe enzyme and receptor mechanisms. Studies to understand the molecular mechanism by which fluorine alters ligand-agonist binding have included the synthesis of several new fluorinated agonist analogues, and now have been extended to probing selective interactions with cloned receptors. New catecholamino-acids have been synthesized that are designed to be prodrugs for selective in vivo response.