Identification of endothelin receptors in cultured cerebellar neurons.
We have described the binding of [125I]endothelin-1 (ET-1) to cultured rat cerebellar granule cells. Binding of [125I]ET-1 was specific, saturable, and time-dependent. Scatchard analysis of saturation binding data indicated a single class of high affinity binding site with a KD of 95 pM, and a Bmax of 8110 receptors/cell. Functionally, the binding of ET-1 stimulated phosphatidylinositide (PI) hydrolysis in a dose- and time-dependent fashion. PI turnover was found to be inhibitable by 1 microM phorbol dibutyrate but not by 1 microgram/ml pertussis toxin, suggesting that the ET-1-mediated response is regulated by protein kinase C and a pertussis toxin-insensitive guanine nucleotide (GTP) binding protein.
Lysko
P G
PG
Department of Pharmacology, Smith Kline Beecham, King of Prussia, PA 19406-0939.
Feuerstein
G
G
Pullen
M
M
Wu
H L
HL
Nambi
P
P
D000818:Animals; D002478:Cells, Cultured; D002531:Cerebellum / Q000378:metabolism*; D016232:Endothelins / Q000378:metabolism*; D007294:Inositol / Q000378:metabolism; D007700:Kinetics; D009474:Neurons / Q000378:metabolism*; D037342:Pertussis Toxin; D015240:Phorbol 12,13-Dibutyrate / Q000494:pharmacology; D010716:Phosphatidylinositols / Q000378:metabolism; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D017466:Receptors, Endothelin; D010566:Virulence Factors, Bordetella / Q000494:pharmacology
D016232:Endothelins; D010716:Phosphatidylinositols; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; D010566:Virulence Factors, Bordetella; D015240:Phorbol 12,13-Dibutyrate; D007294:Inositol; D037342:Pertussis Toxin