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alpha(2)-Adrenoceptor subtypes-mediated physiological, pharmacological actions.

机译:alpha(2)-肾上腺素受体亚型介导的生理,药理作用。

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摘要

alpha(2)-Adrenoceptors are involved in various physiological functions, particularly in the cardiovascular system and the central nervous system. Different adrenoceptor subtypes (alpha(2A), alpha(2B) and alpha(2C)) have been recognised and the different subtypes may have role in activation of distinct physiological and pharmacological pathways. Some of the actions of alpha(2)-adrenoceptor stimulants are likely to be mediated exclusively by alpha(2A)-adrenoceptor subtype, like antihypertensive and bradycardic effects. alpha(2A)-Adrenoceptor may have dominant role in sedative and hypothermic actions, in inhibition of gastric acid secretion and gastric motor activity, as well as in stabilisation of thrombus. Besides alpha(2A)-adrenergic receptors alpha(2B) and alpha(2C)-adrenoceptor subtypes may also be involved in some of the classical effects of alpha(2)-adrenoceptor stimulants, like in presynaptic regulation of transmitter release and antinociceptive action. alpha(2B)-Adrenoceptor has dominant role in the vasoconstrictor effect of alpha(2)-adrenoceptor agonists, and its activation induces contraction of rat uterus in late pregnancy. alpha(2B)-Adrenoceptor mediates gastric mucosal protective action initiated centrally in the rat, as well as it may have role also in developmental or reproductive processes. alpha(2C)-Adrenoceptor subtypes may be involved in stress-dependent depression and other psychiatric illnesses like attention deficit hyperactivity disorder-together with alpha(2A)-adrenoceptor. alpha(2C)-Adrenergic receptors seem to mediate peripheral actions as well, like venous vasoconstriction. Identification of separate physiological roles for different alpha(2)-adrenergic receptor subtypes could improve design of novel compounds for specific therapeutic goals.
机译:alpha(2)-肾上腺素受体参与各种生理功能,特别是在心血管系统和中枢神经系统中。已经认识到不同的肾上腺素能受体亚型(alpha(2A),alpha(2B)和alpha(2C)),并且不同的亚型可能在不同的生理和药理途径的激活中起作用。 alpha(2)-肾上腺素受体兴奋剂的某些作用很可能仅由alpha(2A)-肾上腺素受体亚型介导,例如降压和心动过缓作用。 alpha(2A)-肾上腺素受体可能在镇静和体温过低,抑制胃酸分泌和胃运动活动以及血栓稳定中起主要作用。除了alpha(2A)-肾上腺素能受体外,alpha(2B)和alpha(2C)-肾上腺素能受体亚型也可能参与了alpha(2)-肾上腺素能刺激物的一些经典作用,如突触前调节递质释放和抗伤害感受作用。 alpha(2B)-肾上腺素受体在alpha(2)-肾上腺素受体激动剂的血管收缩作用中起主要作用,其激活可诱导妊娠晚期大鼠子宫的收缩。 alpha(2B)-肾上腺素能受体介导大鼠中央发起的胃粘膜保护作用,并且它也可能在发育或生殖过程中起作用。 alpha(2C)-肾上腺素受体亚型可能与压力依赖性抑郁症和其他精神疾病(例如注意力不足过动症)和alpha(2A)-肾上腺素能受体有关。 α(2C)-肾上腺素能受体似乎也介导外周动作,如静脉血管收缩。识别不同的alpha(2)-肾上腺素受体亚型的单独的生理作用可以改善针对特定治疗目标的新型化合物的设计。

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