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SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL PROFILE OF TROPICAMIDE ENANTIOMERS

机译:对乙酰氨基化物对映体的合成,表征和药理学特征

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The synthesis, chemical characterization and antimuscarinic activity of the two enantiomers of tropicamide are reported. Functional (rabbit vas deferens, guinea pig heart (force) and ileum) as well as binding experiments (m(1) and m(4) human muscarinic receptors expressed in CHO-K1 cells; M(2) and M(3) receptors of rat heart and submaxillary gland membranes) were used to evaluate the antimuscarinic activity of the enantiomers. The results show that none of the enantiomers is able to significantly discriminate among the receptors studied and therefore do not support the proposal of tropicamide as an M(4) (m(4)) selective agent. [References: 27]
机译:报道了托吡酰胺的两种对映异构体的合成,化学表征和抗毒蕈碱活性。功能性(兔输精管,豚鼠心脏(力)和回肠)以及结合实验(在CHO-K1细胞中表达的人毒蕈碱受体(m(1)和m(4)); M(2)和M(3)受体(大鼠心脏和上颌下腺膜的抗性)用于评估对映异构体的抗毒蕈碱活性。结果表明,没有一种对映异构体能够明显区分所研究的受体,因此不支持将tropicamide作为M(4)(m(4))选择剂的提议。 [参考:27]

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