受容体刺激後の細胞応答 : 創薬における薬理学の役割 ―創薬のための薬物効果判定とその作用機作研究モデル―

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When cellular stimulants such as neurotransmitters, hormones, autacoids, cytokines and growth factors stimulate their respective specific receptors in the plasma membranes of cells, a variety of responses are elicited. GTP-binding proteins are also involved in the reactions between receptors and cellular effectors. Stimulation of receptors are subsequently coupled to the activation of ion channels, turnover of inositol phospholipid metabolism, adenylate cyclase and guanylate cyclase, inhibition of adenylate cyclase and potentiation of all proliferation. Active substances such as the so-called second messengers are produced in the cells. In this article, two findings are described: 1) Ca<SUP>2+</SUP>, which increases by stimulation of receptors with neurotransmitters and hormones, stimulated Ca<SUP>2+</SUP>/calmodulin-dependent protein kinase II in cell systems such as NG108-15 neuroblastoma × glioma hybrid cells and primarily cultured neuronal cells of rat hippocampus. 2) Coupling preferences and possible transduction mechanisms from experiments on NG108-15 cells and NL308 neuroblastoma × fibroblast hybrid cells which have been stably transfected with DNA for ml, m2, m3 and m4 muscarinic acetylcholine receptors were examined. These results may provide a useful research model for examining and evaluating the effects and mechanisms of the drugs on a living system and may help develop useful methodology for the discovery of innovative drugs.
社団法人日本薬理学会の論文

受容体刺激後の細胞応答 : 創薬における薬理学の役割 ―創薬のための薬物効果判定とその作用機作研究モデル―

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