Two Different Endothelin B Receptor Subtypes Mediate Contraction of the Rabbit Saphenous Vein

The Japanese Journal of Pharmacology

Mariko Nishiyama⁴  Li-Hua Shan⁴  Kayoko Moroi⁴  Masao Yamamoto¹  Chikahisa Takasaki³  Tomoh Masaki²  Sadao Kimura⁴ 

[1] Research Laboratories, Nippon Chemiphar Co., Ltd.;Department of Pharmacology, Faculty of Medicine, Kyoto University;Department of Chemistry, Faculty of Science, Tohoku University;Division of Cardiovascular Biology, Center for Biomedical Science, Chiba University School of Medicine

关键词: Endothelin;    Sarafotoxin;    Saphenous artery and vein (rabbit);    Endothelin receptor;    Endothelin receptor antagonist;   

DOI  :  10.1254/jjp.68.235

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(27)Cited-By(15)To study endothelin receptor subtypes that mediate venous smooth muscle contraction, effects of some endothelin receptor agonists and antagonists on the rabbit lateral saphenous vein were examined and compared with those on the saphenous artery. In the artery, endothelin (ET)-1 elicited concentration-dependent contractions, while selective ETB-receptor agonists, IRL1620 (Suc-[Glu9, Ala11, 15]ET-1(8-21)) and sarafotoxin 6c (S6c) had almost no effect. The ET-1-induced responses shifted in parallel to the right by BQ-123 (cyclo (-D-Trp-D-Asp-Pro-D-Val-Leu-)), an ETA-receptor antagonist, or PD142893 (Ac-D-Dip-Leu-Asp-Ile-Ile-Trp), an ETA/ETB-receptor antagonist, indicating the involvement of the ETA receptor in this response. In the saphenous vein, not only ET-1 and ET-3, but also ETB-receptor agonists, IRL1620, S6c and [Glu9jsarafotoxin 6b ([Glu9]S6b), produced concentration-dependent, BQ-123-insensitive contractions. PD142893 did not affect the ET-1-induced contraction, but it shifted greatly the IRL1620-induced concentration-response curve in parallel to the right. The major components of ET-3-, S6c- and [Glu9]S6b-induced contractions were resistant to PD142893. These results indicate that two different vasoconstrictive ETB-receptor subtypes, ETB, (sensitive to IRL 1620 and PD 142893) and ETB2 (insensitive to IRL 1620 and PD 142893), are located on the smooth muscle of the saphenous vein.

【 授权许可】

Unknown