Prospective Study of Sarpogrelate Hydrochloride on Patients with Arterioscler　osis Obliterans

Ren, Shiyan; Qian, Songyi; Wang, Wei; Liu, Jiagtao; Liu, Peng

doi:10.5761/atcs.oa.12.02061

Cited by 12 publications

(5 citation statements)

References 16 publications

(23 reference statements)

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“…These chronic effects combined with a reduction of 5-HT and angiotensin II-induced vascular smooth muscle cell proliferation (Sharma, et al, 2001;Watanabe, et al, 2001) could limit vascular remodeling. This is now clear for peripheral arterial disease in which sarpogrelate improves outcome of symptomatic patients (Ren, et al, 2013) but it remains to be demonstrated after endovascular therapy. Retrospective studies showed a reduction of major clinical endpoints such as amputation or death from any cause after endovascular therapy for critical hindlimb ischemia (Takahara, et al, 2014) and the first preliminary results of a recent prospective study suggest that sarpogrelate associated to aspirin is as efficacious as sarpogrelate associated to clopidogrel for the prevention of restenosis following femoropopliteal arterial stenting (Chen, et al, 2015).…”

Section: Vascular Tone Of Systemic and Coronary Arteriesmentioning

confidence: 99%

New therapeutic opportunities for 5-HT2 receptor ligands

Maroteaux

Ayme-Dietrich

Aubertin-Kirch

et al. 2017

Pharmacology & Therapeutics

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Serotonergic dysfunction is mainly associated with neuropsychiatric and cardiovascular disorders but has also been linked with many other pathological conditions. Serotonin (5-hydroxytryptamine, 5-HT) mediates numerous physiological functions in the brain and the periphery by activating a variety of receptors. 5-HT receptors are divided into four classes, three of which belong to the G protein-coupled receptor family. This review provides an overview of the recent pharmacological developments involving the Gq-coupled 5-HT receptor subfamily as well as the pathological implications of this receptor subfamily with regard to fibrosis, the central nervous system, cardiovascular disorders, and cancer. The final section highlights new therapeutic opportunities and emerging research revealing unexplored medical opportunities for this class of 5-HT receptors. The development of biased 5-HT receptor ligands appears to be an interesting topic in various areas. In light of recent discoveries, the need for the development of new and safer drugs should take into account the risk of cardiovascular side effects such as pulmonary hypertension and heart valve disease.

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Section: Vascular Tone Of Systemic and Coronary Arteriesmentioning

confidence: 99%

New therapeutic opportunities for 5-HT2 receptor ligands

Maroteaux

Ayme-Dietrich

Aubertin-Kirch

et al. 2017

Pharmacology & Therapeutics

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“…Blockage of the 5-HT2A receptor by the antagonist sarpogrelate retards the progression of atherosclerosis in a rabbit model by upregulation of eNOS and presumably antiproliferative effects on smooth muscle cells and macrophages [45]. Consistent with these findings, sarpogrelate has a therapeutic effect an patients with atherosclerosis obliterans [46] and critical limb ischemia [47]. In a collective of diabetic patients, sarpogrelate decreased coronary artery plaque volume [48].…”

Section: Serotonin In Atherosclerosismentioning

confidence: 70%

Serotonin: a platelet hormone modulating cardiovascular disease

Rieder

Gauchel

Bode

et al. 2020

J Thromb Thrombolysis

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Cardiovascular diseases and depression are significant health burdens and increasing evidence suggests a causal relationship between them. The incidence of depression among patients suffering from cardiovascular disease is markedly elevated, and depression itself is an established cardiovascular risk factor. Serotonin 5-hydroxytryptamin (5-HT), a biogenic amine acting as a neurotransmitter and a peripheral hormone, is involved in the pathogenesis of both, cardiovascular disease and depression. Novel cardiovascular functions of 5-HT have recently been described and will be summarized in this review. 5-HT has a broad spectrum of functions in the cardiovascular system, yet the clinical or experimental data are partly conflicting. There is further research needed to characterize the clinical effects of 5-HT in particular tissues to enable targeted pharmacological therapies.

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“…A 5-HT2R antagonist, sarpogrelate, 43 which inhibited platelet aggregation and thrombus formation [44][45][46][47] was introduced as a therapeutic agent for the treatment of vascular occlusive disease [48][49][50][51] and for patients undergoing percutaneous interventions. 52,53 In a porcine model, sarpogrelate inhibited 5-HT-induced coronary contraction and spam.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of 5‐Hydroxytryptamine Receptor 2B Reduced Vascular Restenosis and Mitigated the β‐Arrestin2–Mammalian Target of Rapamycin/p70S6K Pathway

Liu

Wang

et al. 2018

JAHA

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BackgroundAs a monoamine neurotransmitter, 5‐hydroxytryptamine (5‐HT) or serotonin modulates mood, appetite, and sleep. Besides, 5‐HT also has important peripheral functions. 5‐HT receptor 2B (5‐HT2BR) plays a key role in cardiovascular diseases, such as pulmonary arterial hypertension and cardiac valve disease. Percutaneous intervention has been used to restore blood flow in occlusive vascular disease. However, restenosis remains a significant problem. Herein, we investigated the role of 5‐HT2BR in neointimal hyperplasia, a key pathological process in restenosis.Methods and ResultsThe expression of 5‐HT2BR was upregulated in wire‐injured mouse femoral arteries. In addition, BW723C86, a selective 5‐HT2BR agonist, promoted the injury response during restenosis. 5‐HT and BW723C86 stimulated migration and proliferation of rat aortic smooth muscle cells. Conversely, LY272015, a selective antagonist, attenuated the 5‐HT–induced smooth muscle cell migration and proliferation. In vitro study showed that the promigratory effects of 5‐HT2BR were mediated through the activation of mammalian target of rapamycin (mTOR)/p70S6K signaling in a β‐arrestin2–dependent manner. Inhibition of mammalian target of rapamycin or p70S6K mitigated 5‐HT2BR–mediated smooth muscle cell migration. Mice with deficiency of 5‐HT2BR showed significantly reduced neointimal formation in wire‐injured arteries.ConclusionsThese results demonstrated that activation of 5‐HT2BR and β‐arrestin2–biased downstream signaling are key pathological processes in neointimal formation, and 5‐HT2BR may be a potential target for the therapeutic intervention of vascular restenosis.

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Prospective Study of Sarpogrelate Hydrochloride on Patients with Arterioscler　osis Obliterans

Abstract: Sarpogrelate has a therapeutic effect on patients with atherosclerotic obliterans.

Cited by 12 publications

References 16 publications

New therapeutic opportunities for 5-HT2 receptor ligands

New therapeutic opportunities for 5-HT2 receptor ligands

Serotonin: a platelet hormone modulating cardiovascular disease

Inhibition of 5‐Hydroxytryptamine Receptor 2B Reduced Vascular Restenosis and Mitigated the β‐Arrestin2–Mammalian Target of Rapamycin/p70S6K Pathway

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Prospective Study of Sarpogrelate Hydrochloride on Patients with Arterioscler osis Obliterans

Abstract: Sarpogrelate has a therapeutic effect on patients with atherosclerotic obliterans.

Cited by 12 publications

References 16 publications

New therapeutic opportunities for 5-HT2 receptor ligands

New therapeutic opportunities for 5-HT2 receptor ligands

Serotonin: a platelet hormone modulating cardiovascular disease

Inhibition of 5‐Hydroxytryptamine Receptor 2B Reduced Vascular Restenosis and Mitigated the β‐Arrestin2–Mammalian Target of Rapamycin/p70S6K Pathway

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Prospective Study of Sarpogrelate Hydrochloride on Patients with Arterioscler　osis Obliterans