Functional expression of 5-HT1c receptor cDNA in COS 7 cells and its influence on protein kinase C.
Two subtypes of receptors for serotonin (5-hydroxytryptamine; 5-HT) are known to stimulate inositol (1,4,5)-trisphosphate production, the 5-HT1c and 5-HT2 receptors. In this study we investigated the ability of 5-HT1c receptors, transiently expressed in COS 7 cells, to functionally interact with protein kinase C-alpha, 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-alpha from the cytosolic to the membrane fraction in a Ca(2+)-dependent manner which was prevented by the 5-HT1c 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+.
Lutz
E M
EM
MRC Brain Metabolism Unit, University Department of Pharmacology, Edinburgh, UK.
Mitchell
R
R
Johnson
M S
MS
MacEwan
D
D
D000818:Animals; D002118:Calcium / Q000502:physiology; D002478:Cells, Cultured; D002522:Chlorocebus aethiops; D003001:Cloning, Molecular; D004247:DNA / Q000235:genetics; D015870:Gene Expression; D066298:In Vitro Techniques; D015240:Phorbol 12,13-Dibutyrate / Q000494:pharmacology; D011493:Protein Kinase C / Q000502:physiology*; D011985:Receptors, Serotonin / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction; D014162:Transfection
D011985:Receptors, Serotonin; D015240:Phorbol 12,13-Dibutyrate; D004247:DNA; D011493:Protein Kinase C; D002118:Calcium