Endothelin-1-induced translocation of RhoA is mediated by endothelin ET(A) receptors in rat bronchial smooth muscle.
To clarify the receptor subtype(s) contributing to the RhoA activation by endothelin-1 in bronchial smooth muscle, the effects of BQ-123 [cycro(D-Asp-Pro-D-Val-Leu-D-Trp)], an endothelin ET(A) receptor antagonist, and/or BQ-788 [2,6-dimethylpiperidinecarbonyl-g-methyl-Leu-Nin-(Methoxycarbonyl)-D-Trp-D-Nle], an endothelin ET(B) receptor antagonist, on the endothelin-1-induced translocation of RhoA to plasma membrane were examined. Incubation of rat bronchial smooth muscle with endothelin-1 induced a distinct translocation of RhoA to plasma membrane, indicating an activation of RhoA by endothelin-1. The endothelin-1-induced translocation of RhoA was completely blocked by treatment with BQ-123, whereas BQ-788 had no effect. Thus, endothelin ET(A) but not ET(B) receptors might be involved in the endothelin-1-induced translocation of RhoA in rat bronchial smooth muscle.
Chiba
Yoshihiko
Y
Department of Pharmacology, School of Pharmacy, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan. chiba@hoshi.ac.jp
Sakai
Hiroyasu
H
Misawa
Miwa
M
D000577:Amides / Q000494:pharmacology; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D015153:Blotting, Western; D001980:Bronchi / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D003600:Cytosol / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D065130:Endothelin A Receptor Antagonists; D065131:Endothelin B Receptor Antagonists; D019332:Endothelin-1 / Q000494:pharmacology*; D066298:In Vitro Techniques; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000494:pharmacology; D009130:Muscle, Smooth / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology; D009842:Oligopeptides / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D021381:Protein Transport / Q000187:drug effects; D011725:Pyridines / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D044022:Receptor, Endothelin A / Q000502:physiology*; D013997:Time Factors; D020742:rhoA GTP-Binding Protein / Q000378:metabolism*
D000577:Amides; D065130:Endothelin A Receptor Antagonists; D065131:Endothelin B Receptor Antagonists; D019332:Endothelin-1; D009125:Muscle Relaxants, Central; D009842:Oligopeptides; D010456:Peptides, Cyclic; D010880:Piperidines; D011725:Pyridines; D044022:Receptor, Endothelin A; C108830:Y 27632; C086539:BQ 788; D001285:Atropine; D020742:rhoA GTP-Binding Protein; C072247:cyclo(Trp-Asp-Pro-Val-Leu); D007213:Indomethacin