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IN VITRO AND IN VIVO EVALUATION OF THE SUBTYPE-SELECTIVE MUSCARINIC AGONIST PD 151832

机译:亚型选择性肌肉激动剂PD 151832的体外和体内评价

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PD 151832 is a potent partial muscarinic agonist that displays a high level of functional selectivity for the muscarinic mi receptor subtype, as evidenced by its selective stimulation of PI turnover and cellular metabolic activity in transfected Hml-CHO cells at concentrations that produce minimal stimulation of other cloned human muscarinic receptors. PD 151832 enhanced the amplification of Hml-transfected NIH-3T3 cells at concentrations lower than those required to produce similar effects in Hm2 or Hm3-transfected cells. The functional mi selectivity of PD 151832 is consistent with its improvement of mouse water maze performance at doses far lower than those required to produce peripheral parasympathetic side effects. [References: 23]
机译:PD 151832是一种有效的部分毒蕈碱激动剂,对毒蕈碱mi受体亚型表现出高水平的功能选择性,这可以通过选择性刺激PI转染和在转染的Hml-CHO细胞中以最小程度刺激其他浓度的细胞代谢活性来证明。克隆的人毒蕈碱受体。 PD 151832以低于在Hm2或Hm3转染的细胞中产生类似作用所需浓度的浓度增强了Hml转染的NIH-3T3细胞的扩增。 PD 151832的功能选择性与它对小鼠水迷宫性能的改善相一致,其剂量远低于产生周围副交感神经副作用所需的剂量。 [参考:23]

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