Does a second generation of centrally acting antihypertensive drugs really exist

作者: Josiane Feldman , Hugues Greney , Laurent Monassier , Catherine Vonthron , Véronique Bruban

DOI: 10.1016/S0165-1838(98)00093-9

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摘要: The site of the hypotensive action imidazoline compounds, such as clonidine, was first identified within rostroventrolateral part brainstem: nucleus reticularis lateralis. After that, it shown that imidazolines and related substances reduced blood pressure when applied in this area whereas catecholamines were not capable producing an effect. These data led us to suggest existence receptors specific for imidazoline-like compounds different from α 2 -adrenoceptors. Soon after, binding sites reported brain a variety peripheral tissues including human kidney. As expected, these do bind catecholamines. are already subclassified two groups: I 1 -subtype sensitive clonidine idazoxan, -subtype, idazoxan nearly insensitive clonidine. Functional studies confirmed effects clonidine-like drugs involved while their most frequent side only However, recent functional evidence suggests cross talk between -adrenoceptors is necessary trigger effect ventral brainstem. Rilmenidine Moxonidine leader new class antihypertensive selective receptors. At doses, devoid significant sedative evoked hypotension injected lateralis region; competed [ 3 H]-clonidine bound medullary membrane preparations but proved more cerebral than It suggested selectivity might explain low incidence effects. Additional potentially beneficial actions on cardiac arrhythmias or congestive heart failure enlarge therapeutic interest imidazoline-related drugs. Recent throw light optimal pharmacological profile second generation centrally acting

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