THE 5‐HT2 RECEPTOR ANTAGONIST SARPOGRELATE REDUCES URINARY AND PLASMA LEVELS OF THROMBOXANE A2 AND URINARY ALBUMIN EXCRETION IN NON‐INSULIN‐DEPENDENT DIABETES MELLITUS PATIENTS†

@article{Ogawa1999THE5R,
  title={THE 5‐HT2 RECEPTOR ANTAGONIST SARPOGRELATE REDUCES URINARY AND PLASMA LEVELS OF THROMBOXANE A2 AND URINARY ALBUMIN EXCRETION IN NON‐INSULIN‐DEPENDENT DIABETES MELLITUS PATIENTS†},
  author={Susumu Ogawa and Kazuhisa Takeuchi and K. Sugimura and C Sato and M Fukuda and R. Lee and Shinya Ito and T. Sato},
  journal={Clinical and Experimental Pharmacology and Physiology},
  year={1999},
  volume={26}
}
  • S. Ogawa, K. Takeuchi, T. Sato
  • Published 1 May 1999
  • Medicine, Biology
  • Clinical and Experimental Pharmacology and Physiology
1. Therapeutic effects of a 5‐HT2 receptor antagonist sarpogrelate on microalbuminuria and thromboxane (TX)A2 biosynthesis were examined in non‐insulin‐dependent diabetes mellitus (NIDDM) patients. 
Persistent insulin-sensitizing effects of sarpogrelate hydrochloride, a serotonin 2A receptor antagonist, in patients with peripheral arterial disease.
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Sarpogrelate has a persistent insulin-sensitizing effect through adiponectin modification and might be beneficial for anti-atherosclerotic therapy, at least, in non-diabetic and non-medicated diabetic patients with PAD.
Sarpogrelate: cardiovascular and renal clinical potential
  • S. Doggrell
  • Medicine, Biology
    Expert opinion on investigational drugs
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Small clinical trials indicate that sarpogrelate may be beneficial in the treatment of coronary artery disease, angina, restenosis, heart valve prostheses surgery, diabetes mellitus, Raynaud's phenomenon, systemic sclerosis and Buerger’s disease.
Blockade of serotonin 2A receptor improves glomerular endothelial function in rats with streptozotocin-induced diabetic nephropathy
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The results indicate that sarpogrelate improves endothelial function in rats with STZ-induced diabetes through a reduction of glomerular platelet activation and an increase in serum adiponectin concentrations and suggest that sargodrelate is potentially useful for the treatment of diabetic nephropathy.
Therapeutic potentials of sarpogrelate in cardiovascular disease.
TLDR
Sarpogrelate, a specific 5-HT2A receptor antagonist, has been found to have beneficial effects in peripheral vascular disease, restenosis after coronary stenting, pulmonary hypertension, acute and chronic myocardial infarction.
Reduced albuminuria with sarpogrelate is accompanied by a decrease in monocyte chemoattractant protein-1 levels in type 2 diabetes.
TLDR
Sarpogrelate can reduce albuminuria and plasma and urinary monocyte chemoattractant protein-1 levels while increasing plasma adiponectin in diabetic nephropathy and these effects seem to be mediated via mechanisms that are different from those of angiotensin II receptor blocker or thiazolidinedione.
The role of 5-HT on the cardiovascular and renal systems and the clinical potential of 5-HT modulation
  • S. Doggrell
  • Medicine, Biology
    Expert opinion on investigational drugs
  • 2003
TLDR
The main peripheral sources of 5-hydroxytryptamine (5-HT) are as a neurotransmitter and local hormone in the gastrointestinal tract, and stored in circulating platelets and pulmonary neuroepithelial bodies, and in diabetes, sarpogrelate may protect against nephropathy.
Blockade of 5-HT2A Receptors by Sarpogrelate Protects the Heart Against Myocardial Infarction in Rats
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The results of this study support the view that serotonin and 5-HT2A may contribute to the deleterious effects of ischemic injury in the heart.
Beneficial Effects of Sarpogrelate Hydrochloride, a 5-ht2a Receptor Antagonist, Supplemented with Pioglitazone on Diabetic Model Mice
TLDR
The results suggest that the combined application of sarpogrelate with pioglitazone provides therapeutic benefits not only in preventing adverse effects but also in the treatment of diabetes.
Diabetes‐induced changes in the 5‐hydroxytryptamine inhibitory receptors involved in the pressor effect elicited by sympathetic stimulation in the pithed rat
TLDR
Experimental diabetes produces changes in the inhibitory effect induced by 5‐HT on electrically induced sympathetic pressor responses, such that the inhibitatory action induced by5‐HT in diabetic pithed rats is mediated by prejunctional 5‐ HT1A receptors.
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TLDR
Dose‐response curves were obtained to bolus injections of 5‐hydroxytryptamine (5‐HT) in Krebs'‐perfused hindquarters of male Wistar rats to study the effects of alloxan‐treated 14 day diabetic rats compared with non‐diabetics.
Increased thromboxane B2 excretion in diabetes mellitus.
TLDR
The results suggest that renal TXA2 synthesis may be augmented in diabetic nephropathy and may play a pathophysiologic role in renal hemodynamics as well as in protein excretion.
Therapeutic effect of sarpogrelate, a new 5-hydroxytryptamine receptor 2A antagonist, on diabetic nephropathy and neuropathy.
TLDR
A clinical evaluation of the usefulness of sarpogrelate in diabetic nephropathy and neuropathy was performed with type II diabetes mellitus patients who gave their informed consent.
Prostacyclin and thromboxane in diabetes.
TLDR
Plasma concentrations of 6-keto-PGF1 alpha and thromboxane B2 were not related to concentrations of glucose, haemoglobin A1, high-density lipoprotein cholesterol, cholesterol, triglycerides, magnesium, or creatinine, and suggest that in diabetics with microangiopathy a balance between prostacyclin and thROMboxane A2 is shifted to dominance by prostacyClin.
Changes in reactivity towards 5‐hydroxytryptamine in the renal vasculature of the diabetic spontaneously hypertensive rat
TLDR
The marked effect of U46619 on the reactivity towards 5-HT in kidneys of diabetic and control rats indicates that this interaction might be important given the increased levels of thromboxane A2 reported to occur in these diseases.
Thromboxane in the pathogenesis of glomerular injury in diabetes.
TLDR
The results support roles for TX in the initiation of, and for TX and/or endoperoxides in the progression of glomerular injury in SDR.
Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzenes.
TLDR
A series of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimental thrombosis in mice, and were found to be potent antagonists to S2 serotonergic receptor.
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