Functional expression of 5‐HT1c receptor cDNA in COS 7 cells and its influence on protein kinase C

[摘要]

Two subtypes of receptors for serotonin (5-hydroxytryptamine; 5-HT) are known to stimulate inositol (l,4,5)-trisphosphate production, the 5-HT_1c and 5-HT₂ receptors. In this study we investigated the ability of 5-HT_1c receptors, transiently expressed in COS 7 cells, to functionally interact with protein kinase C-α, the indigenous (phorbol ester-responsive) isoform of the enzyme in those cells. Serotonin caused translocation of the [³H]phorbol 12,13-dibutyrate (PDBu) binding site of PKC-α from the cytosolic to the membrane fraction in a Ca²⁺-dependent manner which was prevented by the 5-HT_1c receptor antagonist mianserin. The lipid activators of PKC, PDBu and 1,2-dioctanoyl-sn-glycerol (DOG) also caused translocation, but through a mechanism apparently quite independent of Ca²⁺

[学科分类] 生物化学/生物物理

[关键词] Serotonin;5-HT1creceptor;Expression;Protein kinase C