van Zwieten P A
Department of Pharmacotherapy, University of Amsterdam, The Netherlands.
Pharm World Sci. 1995 Nov 24;17(6):186-90. doi: 10.1007/BF01870609.
Imidazoline (I1)-receptors in the central nervous system play a role in the central regulation of blood pressure and heart rate. Stimulation of these receptors in the rostral ventrolateral medulla induces peripheral sympathoinhibition, and hence a reduction of elevated blood pressure. The imidazoline derivatives moxonidine and rilmenidine are moderately selective I1 receptor stimulants which have been introduced as centrally acting antihypertensives. Since they have little affinity for alpha 2-adrenoceptors, they may be expected to cause less sedation and dry mouth than the alpha 2-adrenoceptor agonists clonidine and methyldopa. The concept of I1 receptors and their agonists therefore offers the possibility to develop centrally acting antihypertensives with a more favourable profile of adverse reactions than the classical alpha 2-adrenoceptor stimulants such as clonidine and methyldopa.
中枢神经系统中的咪唑啉（I1）受体在血压和心率的中枢调节中发挥作用。刺激延髓头端腹外侧的这些受体可诱导外周交感神经抑制，从而降低升高的血压。咪唑啉衍生物莫索尼定和利美尼定是中度选择性I1受体激动剂，已作为中枢性抗高血压药引入。由于它们对α2肾上腺素能受体的亲和力很小，因此预计它们引起的镇静和口干比α2肾上腺素能受体激动剂可乐定和甲基多巴要少。因此，I1受体及其激动剂的概念为开发不良反应比可乐定和甲基多巴等经典α2肾上腺素能兴奋剂更有利的中枢性抗高血压药提供了可能性。
