کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2563017 | 1127342 | 2006 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Anti-platelet activity of KR-32560, a novel sodium/hydrogen exchanger-1 inhibitor
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موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
داروشناسی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We investigated the anti-platelet effect of a newly synthesized guanidine derivative KR-32560, a sodium/hydrogen exchanger-1 (NHE-1) inhibitor, together with the elucidation of the possible mode of action. KR-32560 concentration dependently inhibited the aggregation of washed rabbit platelets induced by collagen (10 μg mLâ1) and arachidonic acid (AA; 100 μM), with IC50 values of 25 and 46 μM, respectively. Whereas, KR-32560 showed weaker potency against aggregation induced by thrombin (0.05 U mLâ1) and U46619 (1 μM), and had no effect on thapsigargin (0.5 μM)- or A23187 (5 μM)-induced platelet aggregation up to 50 μM. KR-32560 inhibited the collagen-induced [3H]AA liberation in a concentration-dependent manner. In addition, KR-32560 significantly suppressed TXB2 formation in AA-exposed platelets, but had no effect on production of PGD2, indicating an inhibitory effect on TXA2 synthase. This finding was supported by a TXA2 synthase assay that KR-32560 inhibited the conversion of PGH2 into TXB2 with a similar magnitude to suppression of TXB2 formation. Furthermore, KR-32560 significantly inhibited the collagen-induced [Ca2+]i mobilization and serotonin secretion. Taken together, these observations suggest that the anti-platelet activity of KR-32560 may be mediated by the inhibition of cytoplasmic Ca2+ mobilization and AA liberation.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pharmacological Research - Volume 53, Issue 3, March 2006, Pages 265-270
Journal: Pharmacological Research - Volume 53, Issue 3, March 2006, Pages 265-270
نویسندگان
Kyung-Sup Lee, Yong-Ri Jin, Jung-Jin Lee, Yong Lim, Dong-Ju Son, Chong-Kil Lee, Kyu-Yang Yi, Sung-Eun Yoo, Hwa-Sup Shin, Yeo-Pyo Yun,