Levin S L
Int J Clin Pharmacol Res. 1986;6(5):429-39.
Dualism in the effects of atropine, and metixene upon the denervated human parotid salivary gland is demonstrated by the fact that they suppress pilocarpine secretion while themselves causing an extremely intense and prolonged salivation. A still stronger cholinolytic, chlorosyle, although causing salivation, blocks paradoxical salivation initiated by atropine and metacine. With respect to the latter ligands, chlorosyle acts as a partial agonist. Dualism in the cholinolytics' effect is conditioned by generation, following chronic enervation of the gland, of cholinoreceptor subpopulations of different functional significance and evolutional maturity. Depending on the length of the cholinoreceptor reactive zone, cholinolytics initiate blockade of some receptors and excitement of others.
阿托品和美替辛对去神经支配的人腮腺唾液腺的作用具有二元性,这一事实表明,它们在抑制毛果芸香碱分泌的同时,自身却会引起极其强烈且持久的唾液分泌。一种更强效的抗胆碱药氯西律,虽然会引起唾液分泌,但却能阻断由阿托品和甲替辛引发的反常唾液分泌。就后一种配体而言,氯西律起到部分激动剂的作用。抗胆碱药作用的二元性是由腺体长期去神经支配后产生的具有不同功能意义和进化成熟度的胆碱能受体亚群所决定的。根据胆碱能受体反应区的长度,抗胆碱药会引发对某些受体的阻断和对其他受体的兴奋。