Literature DB >> 22659587

K-134, a phosphodiesterase 3 inhibitor, improves gait disturbance and hindlimb blood flow impairment in rat peripheral artery disease models.

Yusuke Sasaki1, Hideo Suzuki, Shinsuke Itoh, Hideo Yoshida, Shoichi Kondo, Keisuke Inoue, Sohei Tanabe.   

Abstract

K-134, a phosphodiesterase 3 (PDE3) inhibitor with anti-thrombotic and anti-hyperplastic activity, is being developed for the treatment of intermittent claudication. We assessed the efficacy of K-134 against gait disturbance in two rat experimental peripheral arterial disease (PAD) models: the bilateral laurate-induced PAD model and femoral artery ligation model. In the laurate-induced peripheral arterial disease model, 1 week of repeated oral administration of K-134 significantly improved gait disturbance. Cilostazol and clopidogrel did not significantly improve gait disturbance. Repeated oral administration of K-134 and cilostazol significantly improved gait disturbance in the femoral artery ligation model. We evaluated the effects of K-134 and cilostazol treatment on hindlimb blood flow pre- and post-treadmill exercise in this model by laser Doppler perfusion imaging. Both drugs increased hindlimb blood flow both pre- and post-treadmill exercise after 1 week of treatment. After 4 weeks of drug treatment, without preceding drug administration which is supposed to exert acute effects on vessel walls, both drugs significantly increased hindlimb blood flow after exercise. Moreover, K-134 at 30 mg/kg significantly prolonged walking distance. These results suggest that K-134 may be useful for treating intermittent claudication.
Copyright © 2012 Elsevier B.V. All rights reserved.

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Year:  2012        PMID: 22659587     DOI: 10.1016/j.ejphar.2012.05.014

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN: 0014-2999            Impact factor:   4.432


  3 in total

1.  Prasugrel, a Platelet P2Y12 Receptor Antagonist, Improves Abnormal Gait in a Novel Murine Model of Thrombotic Hindlimb Ischemia.

Authors:  Kousaku Ohno; Atsuyuki Tomizawa; Makoto Mizuno; Joseph A Jakubowski; Atsuhiro Sugidachi
Journal:  J Am Heart Assoc       Date:  2016-04-06       Impact factor: 5.501

2.  K-134, a phosphodiesterase 3 inhibitor, reduces vascular inflammation and hypoxia, and prevents rupture of experimental abdominal aortic aneurysms.

Authors:  Naoki Unno; Hiroki Tanaka; Tatsuro Yata; Takafumi Kayama; Yuta Yamanaka; Hajime Tsuyuki; Masaki Sano; Kazunori Inuzuka; Ena Naruse; Hiroya Takeuchi
Journal:  JVS Vasc Sci       Date:  2020-10-22

3.  K-134, a phosphodiesterase 3 inhibitor, prevents brain damage by inhibiting thrombus formation in a rat cerebral infarction model.

Authors:  Hideo Yoshida; Yuka Ashikawa; Shinsuke Itoh; Takashi Nakagawa; Akimune Asanuma; Sohei Tanabe; Yoshihiro Inoue; Hiroyoshi Hidaka
Journal:  PLoS One       Date:  2012-10-23       Impact factor: 3.240

  3 in total

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