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135159-51-2,MFCD00887582
Catalog No.:AA00ILMX

135159-51-2 | Sarpogrelate hydrochloride

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5mg
95%
in stock  
$45.00   $32.00
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25mg
95%
in stock  
$153.00   $107.00
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50mg
95%
in stock  
$270.00   $189.00
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100mg
95%
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$369.00   $258.00
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00ILMX
Chemical Name:
Sarpogrelate hydrochloride
CAS Number:
135159-51-2
Molecular Formula:
C24H32ClNO6
Molecular Weight:
465.9670
MDL Number:
MFCD00887582
SMILES:
COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C.Cl
Properties
Computed Properties
 
Complexity:
540  
Covalently-Bonded Unit Count:
2  
Heavy Atom Count:
32  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
14  
Undefined Atom Stereocenter Count:
1  

Literature

Title: Inhibitory Effect of Serotonin Antagonist on Leukocyte-Endothelial Interactions In Vivo and In Vitro.

Journal: PloS one 20160101

Title: Pravastatin and Sarpogrelate Synergistically Ameliorate Atherosclerosis in LDLr-Knockout Mice.

Journal: PloS one 20160101

Title: Beneficial Effects of Sarpogrelate and Rosuvastatin in High Fat Diet/Streptozotocin-Induced Nephropathy in Mice.

Journal: PloS one 20160101

Title: Sarpogrelate hydrochloride, a serotonin 5HT2A receptor antagonist, ameliorates the development of chronic hypoxic pulmonary hypertension in rats.

Journal: Journal of anesthesia 20151001

Title: Effects of serotonin on expression of the LDL receptor family member LR11 and 7-ketocholesterol-induced apoptosis in human vascular smooth muscle cells.

Journal: Biochemical and biophysical research communications 20140418

Title: Selective inhibition of cytochrome P450 2D6 by Sarpogrelate and its active metabolite, M-1, in human liver microsomes.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20140101

Title: A 5-hydroxytryptamine receptor antagonist, sarpogrelate, reduces renal tubulointerstitial fibrosis by suppressing PAI-1.

Journal: American journal of physiology. Renal physiology 20131215

Title: Glucuronidation of a sarpogrelate active metabolite is mediated by UDP-glucuronosyltransferases 1A4, 1A9, and 2B4.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20130801

Title: Sarpogrelate inhibits the expression of ICAM-1 and monocyte-endothelial adhesion induced by high glucose in human endothelial cells.

Journal: Molecular and cellular biochemistry 20130101

Title: Suppression of high lipid diet induced by atherosclerosis sarpogrelate.

Journal: Journal of cellular and molecular medicine 20121001

Title: Effects of sarpogrelate hydrochloride on skin ulcers and quality of life in patients with systemic sclerosis.

Journal: The Journal of dermatology 20120601

Title: Role of serotonin in angiogenesis: induction of angiogenesis by sarpogrelate via endothelial 5-HT1B/Akt/eNOS pathway in diabetic mice.

Journal: Atherosclerosis 20120201

Title: Evaluation of the effectiveness of sarpogrelate on the surrogate markers for macrovascular complications in patients with type 2 diabetes.

Journal: Endocrine journal 20120101

Title: Serotonin potentiates high-glucose-induced endothelial injury: the role of serotonin and 5-HT(2A) receptors in promoting thrombosis in diabetes.

Journal: Journal of pharmacological sciences 20120101

Title: Mechanism of inverse agonist action of sarpogrelate at the constitutively active mutant of human 5-HT2A receptor revealed by molecular modeling.

Journal: Biological & pharmaceutical bulletin 20120101

Title: Effects of additional treatment of sarpogrelate to aspirin therapy on platelet aggregation and plasma plasminogen activator inhibitor activity in patients with stable effort angina.

Journal: Thrombosis research 20111201

Title: Characteristics of the actions by which 5-HT affects electrical and mechanical activities in rabbit jugular vein.

Journal: British journal of pharmacology 20111001

Title: Sarpogrelate protects against high glucose-induced endothelial dysfunction and oxidative stress.

Journal: International journal of cardiology 20110317

Title: Mechanism of sarpogrelate action in improving cardiac function in diabetes.

Journal: Journal of cardiovascular pharmacology and therapeutics 20110101

Title: Relative contributions of 5-hydroxytryptamine (5-HT) receptor subtypes in 5-HT-induced vasoconstriction of the distended human saphenous vein as a coronary artery bypass graft.

Journal: Biological & pharmaceutical bulletin 20110101

Title: Validated LC-MS/MS method for the determination of sarpogrelate in human plasma: application to a pharmacokinetic and bioequivalence study in Chinese volunteers.

Journal: Journal of pharmaceutical and biomedical analysis 20101102

Title: Liquid chromatography tandem mass spectrometry method for the quantification of sarpogrelate, a selective 5-HT(₂A) receptor antagonist, in plasma: application to a pre-clinical pharmacokinetic study.

Journal: Biomedical chromatography : BMC 20101101

Title: Controversies and future perspectives of antiplatelet therapy in secondary stroke prevention.

Journal: Journal of cellular and molecular medicine 20101001

Title: Erythrocyte-protective effect of sarpogrelate hydrochloride (Anplag ®), a selective 5-HT2 receptor antagonist: an in vitro study.

Journal: Journal of artificial organs : the official journal of the Japanese Society for Artificial Organs 20100901

Title: Comparison of antiplatelet potency of sarpogrelate, aspirin, and beraprost in healthy volunteers according to in-vitro closure time.

Journal: Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20100401

Title: Sarpogrelate hydrochloride, a selective 5-hydroxytryptamine(2A) antagonist, augments autologous bone marrow mononuclear cell implantation-induced improvement in endothelium-dependent vasodilation in patients with critical limb ischemia.

Journal: Journal of cardiovascular pharmacology 20100101

Title: Development of sarpogrelate external preparation for intractable pain control. I. Pre-formulation study on application of modified beta-cyclodextrins.

Journal: Chemical & pharmaceutical bulletin 20100101

Title: Case of livedoid vasculopathy with peripheral neuropathy successfully treated with low-dose warfarin.

Journal: The Journal of dermatology 20100101

Title: Study design of SEASON registry: prospective Surveillance of cardiovascular Events in an Antiplatelet-treated arterioSclerosis Obliterans patients in JapaN )SEASON).

Journal: International heart journal 20100101

Title: The prevention of contrast induced nephropathy by sarpogrelate in patients with chronic kidney disease: a study protocol for a prospective randomized controlled clinical trial.

Journal: Trials 20100101

Title: Chronic treatment of hydroxytryptamine type 2a receptor antagonist sarpogrelate hydrochloride modulates the vasoreactivity of serotonin in experimental rabbit vein grafts.

Journal: Journal of vascular surgery 20090901

Title: Sarpogrelate versus aspirin in secondary prevention of cerebral infarction: differential efficacy in diabetes? Subgroup analysis from S-ACCESS.

Journal: Stroke 20090801

Title: Assessment of binding affinity to 5-hydroxytryptamine 2A (5-HT2A) receptor and inverse agonist activity of naftidrofuryl: comparison with those of sarpogrelate.

Journal: Journal of pharmacological sciences 20090801

Title: Acute effects of sarpogrelate, a 5-HT2A receptor antagonist on cytokine production in endotoxin shock model of rats.

Journal: European journal of pharmacology 20090701

Title: Sarpogrelate hydrochloride reduced intimal hyperplasia in experimental rabbit vein graft.

Journal: Journal of vascular surgery 20090501

Title: Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice.

Journal: Endocrine research 20090101

Title: Sarpogrelate-Aspirin Comparative Clinical Study for Efficacy and Safety in Secondary Prevention of Cerebral Infarction (S-ACCESS): A randomized, double-blind, aspirin-controlled trial.

Journal: Stroke 20080601

Title: Comparison of sarpogrelate and ticlopidine in bare metal coronary stent implantation.

Journal: International journal of cardiology 20080507

Title: Blockade of serotonin 2A receptor improves glomerular endothelial function in rats with streptozotocin-induced diabetic nephropathy.

Journal: Clinical and experimental nephrology 20080401

Title: New therapeutic approach for impaired arteriogenesis in diabetic mouse hindlimb ischemia.

Journal: Circulation journal : official journal of the Japanese Circulation Society 20080401

Title: Antiplatelet therapy mitigates cardiac remodeling and dysfunction in congestive heart failure due to myocardial infarction.

Journal: Canadian journal of physiology and pharmacology 20080401

Title: Reduced albuminuria with sarpogrelate is accompanied by a decrease in monocyte chemoattractant protein-1 levels in type 2 diabetes.

Journal: Clinical journal of the American Society of Nephrology : CJASN 20080301

Title: The effects of a 5-HT2A receptor antagonist on blood flow in lumbar disc herniation: application of nucleus pulposus in a canine model.

Journal: European spine journal : official publication of the European Spine Society, the European Spinal Deformity Society, and the European Section of the Cervical Spine Research Society 20080201

Title: Antiplatelet agents sarpogrelate and cilostazol affect experimentally-induced ventricular arrhythmias and mortality.

Journal: Cardiovascular toxicology 20080101

Title: Identification of a key amino acid of the human 5-HT(2B) serotonin receptor important for sarpogrelate binding.

Journal: Journal of pharmacological sciences 20070701

Title: Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease.

Journal: Journal of cardiovascular pharmacology 20070401

Title: Synthesis and 5-HT2A, 5-HT1A and alpha1-binding affinities of 2-[2-Hydroxy-3-(pyridin-3-yl-methyl)amino]-, 2-[2-hydroxy-3-(2-pyridin-2-yl-ethyl)amino]- and 2-[2-hydroxy-3-(4-N-methyl-piperazin-1-yl)-amino]propoxybenzaldehyde-O-(substituted) benzyl oximes.

Journal: Archiv der Pharmazie 20070301

Title: Sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, attenuates neurogenic pain induced by nucleus pulposus in rats.

Journal: Spine 20070201

Title: Marked improvement with sildenafil in a patient with idiopathic pulmonary arterial hypertension unresponsive to beraprost and sarpogrelate.

Journal: Internal medicine (Tokyo, Japan) 20070101

Title: Effect of sarpogrelate, a 5-HT(2A) antagonist, on platelet aggregation in patients with ischemic stroke: clinical-pharmacological dose-response study.

Journal: Cerebrovascular diseases (Basel, Switzerland) 20070101

Title: Increased hypothalamic 5-HT2A receptor gene expression and effects of pharmacologic 5-HT2A receptor inactivation in obese Ay mice.

Journal: Biochemical and biophysical research communications 20061229

Title: Persistent insulin-sensitizing effects of sarpogrelate hydrochloride, a serotonin 2A receptor antagonist, in patients with peripheral arterial disease.

Journal: Circulation journal : official journal of the Japanese Circulation Society 20061101

Title: Induction of indefinite survival of fully mismatched cardiac allografts and generation of regulatory cells by sarpogrelate hydrochloride.

Journal: Transplantation 20061027

Title: Inverse agonist activity of sarpogrelate, a selective 5-HT2A-receptor antagonist, at the constitutively active human 5-HT2A receptor.

Journal: Journal of pharmacological sciences 20061001

Title: 5-HT2 receptor blocker sarpogrelate prevents downregulation of antiapoptotic protein Bcl-2 and protects the heart against ischemia-reperfusion injury.

Journal: Life sciences 20060927

Title: Combined treatment of sustained-release basic fibroblast growth factor and sarpogrelate enhances collateral blood flow effectively in rabbit hindlimb ischemia.

Journal: Circulation journal : official journal of the Japanese Circulation Society 20060901

Title: Identification of amino acid residues important for sarpogrelate binding to the human 5-hydroxytryptamine2A serotonin receptor.

Journal: Journal of pharmacological sciences 20060901

Title: Site-directed mutagenesis of the serotonin 5-Hydroxytryptamine2c receptor: identification of amino acids responsible for sarpogrelate binding.

Journal: Biological & pharmaceutical bulletin 20060801

Title: [Effect of sarpogrelate in enteral feeding of patients with gastroesophageal reflux (GER)].

Journal: Nihon Ronen Igakkai zasshi. Japanese journal of geriatrics 20060701

Title: Homology modelling of the serotoninergic 5-HT2c receptor.

Journal: Journal of enzyme inhibition and medicinal chemistry 20060601

Title: Peripheral 5-HT2A receptor antagonism attenuates primary thermal hyperalgesia and secondary mechanical allodynia after thermal injury in rats.

Journal: Pain 20060501

Title: Sarpogrelate, a 5-hT2A receptor antagonist in intermittent claudication. A phase II European study.

Journal: Vascular medicine (London, England) 20060501

Title: A new method for assessment of an anti-5HT(2A) agent, sarpogrelate hydrochloride, on platelet aggregation.

Journal: Journal of thrombosis and haemostasis : JTH 20060201

Title: Effects of sarpogrelate hydrochloride in a patient with chronic graft-versus-host disease: a case report.

Journal: American journal of hematology 20060201

Title: Inhibition of 5-hydroxytryptamine receptor prevents occlusive thrombus formation on neointima of the rabbit femoral artery.

Journal: Journal of thrombosis and haemostasis : JTH 20060101

Title: Sarpogrelate hydrochloride, an antagonist of 5-hydroxytryptamine receptor, improves skin flap survival and suppresses thrombus formation in injured microvessels of rabbits.

Journal: Journal of reconstructive microsurgery 20060101

Title: The 5-hydroxytryptamine2A receptor antagonist sarpogrelate hydrochloride inhibits acute platelet aggregation in injured endothelium.

Journal: The Journal of international medical research 20060101

Title: Livedo racemosa as a cutaneous manifestation of polycythemia vera.

Journal: European journal of dermatology : EJD 20060101

Title: Contribution of the peripheral 5-HT 2A receptor to mechanical hyperalgesia in a rat model of neuropathic pain.

Journal: Neurochemistry international 20051101

Title: 5-HT2A receptor antagonist increases circulating adiponectin in patients with type 2 diabetes.

Journal: Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20050901

Title: Effects of a 5-HT2A receptor antagonist, sarpogrelate on thermal or inflammatory pain.

Journal: European journal of pharmacology 20050523

Title: New treatment of lumbar disc herniation involving 5-hydroxytryptamine2A receptor inhibitor: a randomized controlled trial.

Journal: Journal of neurosurgery. Spine 20050401

Title: Protective effects of sarpogrelate, a 5-HT2A antagonist, against postischemic myocardial dysfunction in guinea-pig hearts.

Journal: Molecular and cellular biochemistry 20050401

Title: Selective blockade of serotonin 5-HT2A receptor increases coronary blood flow via augmented cardiac nitric oxide release through 5-HT1B receptor in hypoperfused canine hearts.

Journal: Journal of molecular and cellular cardiology 20041201

Title: Effects of 5-HT2A receptor antagonist on blood flow in chronically compressed nerve roots.

Journal: Journal of the peripheral nervous system : JPNS 20041201

Title: Sarpogrelate: cardiovascular and renal clinical potential.

Journal: Expert opinion on investigational drugs 20040701

Title: Effect of sarpogrelate hydrochloride, a 5-HT2 blocker, on insulin resistance in Otsuka Long-Evans Tokushima fatty rats (OLETF rats), a type 2 diabetic rat model.

Journal: Journal of cardiovascular pharmacology 20040201

Title: Sarpogrelate, a 5-HT2 receptor blocker, may have a preconditioning-like effect in patients with coronary artery disease.

Journal: Circulation journal : official journal of the Japanese Circulation Society 20040101

Title: Therapeutic potentials of sarpogrelate in cardiovascular disease.

Journal: Cardiovascular drug reviews 20040101

Title: Effect of the serotonin blocker sarpogrelate on circulating interleukin-18 levels in patients with diabetes and arteriosclerosis obliterans.

Journal: The Journal of international medical research 20040101

Title: Electroencephalographical effects of sarpogrelate hydrochloride versus ticlopidine hydrochloride in elderly patients with peripheral atherosclerosis.

Journal: The Journal of international medical research 20040101

Title: Serotonin receptor antagonist inhibits monocrotaline-induced pulmonary hypertension and prolongs survival in rats.

Journal: Cardiovascular research 20031201

Title: Attenuation of the serotonin-induced increase in intracellular calcium in rat aortic smooth muscle cells by sarpogrelate.

Journal: Canadian journal of physiology and pharmacology 20031101

Title: [Molecular pharmacology of sarpogrelate].

Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20031101

Title: A novel serotonin blocker, sarpogrelate, increases circulating adiponectin levels in diabetic patients with arteriosclerosis obliterans.

Journal: Diabetes care 20030801

Title: Effect of sarpogrelate on altered STZ-diabetes induced cardiovascular responses to 5-hydroxytryptamine in rats.

Journal: Molecular and cellular biochemistry 20030701

Title: Efficacy of serotonin receptor blocker for symptomatic lumbar disc herniation.

Journal: Clinical orthopaedics and related research 20030601

Title: Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling.

Journal: Life sciences 20030530

Title: The role of 5-HT on the cardiovascular and renal systems and the clinical potential of 5-HT modulation.

Journal: Expert opinion on investigational drugs 20030501

Title: Sarpogrelate HCl, a selective 5-HT2A antagonist, retards the progression of atherosclerosis through a novel mechanism.

Journal: Atherosclerosis 20030501

Title: Effect of MCI-9042, a 5-HT2 receptor antagonist, on retinal ganglion cell death and retinal ischemia.

Journal: Experimental eye research 20030401

Title: Sarpogrelate treatment reduces restenosis after coronary stenting.

Journal: American heart journal 20030301

Title: The effects of vasodilators on the relaxation of guinea-pig aorta during acute recoil.

Journal: International journal of cardiology 20021201

Title: Sarpogrelate hydrochloride, a serotonin2A receptor antagonist, reduces albuminuria in diabetic patients with early-stage diabetic nephropathy.

Journal: Diabetes research and clinical practice 20021101

Title: The role of serotonin in ischemic cellular damage and the infarct size-reducing effect of sarpogrelate, a 5-hydroxytryptamine-2 receptor blocker, in rabbit hearts.

Journal: Journal of the American College of Cardiology 20021002

Title: 5-HT2A receptor subtype in the peripheral branch of sensory fibers is involved in the potentiation of inflammatory pain in rats.

Journal: Pain 20020901

Title: Effectiveness of a novel serotonin blocker, sarpogrelate, for patients with angina pectoris.

Journal: American heart journal 20020801

Title: Effects of sarpogrelate, a novel 5-HT2 antagonist, on 5-HT-induced endothelium-dependent relaxations in porcine coronary artery.

Journal: Japanese journal of pharmacology 20020801

Title: Binding and functional affinity of sarpogrelate, its metabolite m-1 and ketanserin for human recombinant alpha-1-adrenoceptor subtypes.

Journal: Pharmacology 20020501

Title: DOI, a 5-HT2 receptor agonist, induces renal vasodilation via nitric oxide in anesthetized dogs.

Journal: European journal of pharmacology 20020215

Title: Effects of chronic administration of sarpogrelate on systolic blood pressure of spontaneously hypertensive rats: comparison with quinapril.

Journal: Pharmacology 20020201

Title: Involvement of rho-kinase in agonists-induced contractions of arteriosclerotic human arteries.

Journal: Arteriosclerosis, thrombosis, and vascular biology 20020201

Title: Sarpogrelate, a specific 5HT2-receptor antagonist, improves the coronary microcirculation in coronary artery disease.

Journal: Clinical cardiology 20020101

Title: [Pharmacological analysis of inhibitory effect of sarpogrelate hydrochloride on human radial artery contraction].

Journal: [Hokkaido igaku zasshi] The Hokkaido journal of medical science 20020101

Title: Blockade of 5-HT(2A) receptors by sarpogrelate protects the heart against myocardial infarction in rats.

Journal: Journal of cardiovascular pharmacology and therapeutics 20020101

Title: [Involvement of peripheral 5-HT2A receptor activation in inflammatory pain].

Journal: Nihon rinsho. Japanese journal of clinical medicine 20010901

Title: Sarpogrelate diminishes changes in energy stores and ultrastructure of the ischemic-reperfused rat heart.

Journal: Canadian journal of physiology and pharmacology 20010901

Title: Effects of sarpogrelate hydrochloride on adenosine diphosphate- or collagen-induced platelet responses in arteriosclerosis obliterans.

Journal: Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis 20010701

Title: Sarpogrelate inhibits serotonin-induced proliferation of porcine coronary artery smooth muscle cells: implications for long-term graft patency.

Journal: The Annals of thoracic surgery 20010601

Title: Monocyte chemotactic protein 1 amplifies serotonin-induced vascular smooth muscle cell proliferation.

Journal: Journal of vascular research 20010101

Title: The effects of sarpogrelate on cardiomyocyte hypertrophy.

Journal: Life sciences 20001103

Title: Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes.

Journal: Archives internationales de pharmacodynamie et de therapie 19960101

Title: In-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-HT2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat tail artery.

Journal: The Journal of pharmacy and pharmacology 19950401

Title: Binding of [3H]haloperidol to dopamine D2 receptors in the rat striatum.

Journal: The Journal of pharmacy and pharmacology 19921101

Title: Rashid M, et, al. Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci. 2003 May 30;73(2):193-207.

Title: Maruyama K, et, al. MCI-9042: high affinity for serotonergic receptors as assessed by radioligand binding assay. J Pharmacobiodyn. 1991 Apr;14(4):177-81.

Title: Kataoka H, et, al. Inhibitory Effect of Serotonin Antagonist on Leukocyte-Endothelial Interactions In Vivo and In Vitro. PLoS One. 2016 Jan 29;11(1):e0147929.

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