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Chemical Compound Review

Sarpogrelate     4-[1-dimethylamino-3-[2-[2- (3...

Synonyms: CHEMBL52939, SureCN49197, CID5160, CHEBI:180532, AC1L1JQL, ...
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Disease relevance of Sarpogrelate


Psychiatry related information on Sarpogrelate


High impact information on Sarpogrelate


Chemical compound and disease context of Sarpogrelate


Biological context of Sarpogrelate


Anatomical context of Sarpogrelate


Associations of Sarpogrelate with other chemical compounds


Gene context of Sarpogrelate


Analytical, diagnostic and therapeutic context of Sarpogrelate

  • The severity score using myocardial perfusion scintigraphy at the same workload was significantly (p < 0.01) decreased by 37% in group B, but not in group A (11%), due to the sarpogrelate treatment [7].
  • Systemic administration of 5-HT2A receptor antagonist (Sarpogrelate HCI) produced analgesic effects on thermal hyperalgesia caused by peripheral inflammation, but failed to attenuate thermal hyperalgesia in chronic constriction injury model [27].
  • Treating the rats with sarpogrelate during reperfusion also showed similar results [24].
  • Otsuka Long-Evans Tokushima Fatty (OLETF) rats, a model of type 2 diabetes, were randomly assigned to 2 groups; those with 30 mg/kg BW/d sarpogrelate treatment of 4 weeks (HTB group) and without (control group) [17].
  • The patients were randomly allocated to two groups, including those receiving oral administration of 200 mg of sarpogrelate (SPG, 8 patients, age 61 +/- 6 years) and those receiving no medication (controls, 7 patients, age 57 +/- 8 years) [28].


  1. 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. Shimizu, Y., Minatoguchi, S., Hashimoto, K., Uno, Y., Arai, M., Wang, N., Chen, X., Lu, C., Takemura, G., Shimomura, M., Fujiwara, T., Fujiwara, H. J. Am. Coll. Cardiol. (2002) [Pubmed]
  2. Functions of 5-HT2A receptor and its antagonists in the cardiovascular system. Nagatomo, T., Rashid, M., Abul Muntasir, H., Komiyama, T. Pharmacol. Ther. (2004) [Pubmed]
  3. Peripheral 5-HT(2A) receptor antagonism attenuates primary thermal hyperalgesia and secondary mechanical allodynia after thermal injury in rats. Sasaki, M., Obata, H., Kawahara, K., Saito, S., Goto, F. Pain (2006) [Pubmed]
  4. Sarpogrelate inhibits serotonin-induced proliferation of porcine coronary artery smooth muscle cells: implications for long-term graft patency. Sharma, S.K., Del Rizzo, D.F., Zahradka, P., Bhangu, S.K., Werner, J.P., Kumamoto, H., Takeda, N., Dhalla, N.S. Ann. Thorac. Surg. (2001) [Pubmed]
  5. Increased hypothalamic 5-HT2A receptor gene expression and effects of pharmacologic 5-HT2A receptor inactivation in obese A(y) mice. Nonogaki, K., Nozue, K., Oka, Y. Biochem. Biophys. Res. Commun. (2006) [Pubmed]
  6. Contribution of the peripheral 5-HT 2A receptor to mechanical hyperalgesia in a rat model of neuropathic pain. Nitanda, A., Yasunami, N., Tokumo, K., Fujii, H., Hirai, T., Nishio, H. Neurochem. Int. (2005) [Pubmed]
  7. Improvement of exercise capacity by sarpogrelate as a result of augmented collateral circulation in patients with effort angina. Tanaka, T., Fujita, M., Nakae, I., Tamaki, S., Hasegawa, K., Kihara, Y., Nohara, R., Sasayama, S. J. Am. Coll. Cardiol. (1998) [Pubmed]
  8. Induction of indefinite survival of fully mismatched cardiac allografts and generation of regulatory cells by sarpogrelate hydrochloride. Akiyoshi, T., Zhang, Q., Inoue, F., Aramaki, O., Hatano, M., Shimazu, M., Kitajima, M., Shirasugi, N., Niimi, M. Transplantation (2006) [Pubmed]
  9. Serotonin receptor antagonist inhibits monocrotaline-induced pulmonary hypertension and prolongs survival in rats. Hironaka, E., Hongo, M., Sakai, A., Mawatari, E., Terasawa, F., Okumura, N., Yamazaki, A., Ushiyama, Y., Yazaki, Y., Kinoshita, O. Cardiovasc. Res. (2003) [Pubmed]
  10. Effects of sarpogrelate hydrochloride in a patient with chronic graft-versus-host disease: a case report. Hayashi, T., Morishita, E., Ontachi, Y., Yamazaki, M., Asakura, H., Yoshida, T., Nakao, S. Am. J. Hematol. (2006) [Pubmed]
  11. The effect of a 5HT2 receptor antagonist sarpogrelate (MCI-9042) treatment on platelet function in Buerger's disease. Rydzewski, A., Urano, T., Hachiya, T., Kaneko, H., Baba, S., Takada, Y., Takada, A. Thromb. Res. (1996) [Pubmed]
  12. Conjunctive effects of the 5HT(2) receptor antagonist, sarpogrelate, on thrombolysis with modified tissue plasminogen activator in different laser-induced thrombosis models. Yamashita, T., Kitamori, K., Hashimoto, M., Watanabe, S., Giddings, J.C., Yamamoto, J. Haemostasis (2000) [Pubmed]
  13. 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. Ogawa, S., Takeuchi, K., Sugimura, K., Sato, C., Fukuda, M., Lee, R., Ito, S., Sato, T. Clin. Exp. Pharmacol. Physiol. (1999) [Pubmed]
  14. Inhibition of serotonin-induced vascular smooth muscle cell proliferation by sarpogrelate. Sharma, S.K., Zahradka, P., Chapman, D., Kumamoto, H., Takeda, N., Dhalla, N.S. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  15. Enhanced serotonin-mediated responses in the nucleus tractus solitarius of spontaneously hypertensive rats. Tsukamoto, K., Sved, A.F., Ito, S., Komatsu, K., Kanmatsuse, K. Brain Res. (2000) [Pubmed]
  16. Effect of sarpogrelate on altered STZ-diabetes induced cardiovascular responses to 5-hydroxytryptamine in rats. Umrani, D.N., Bodiwala, D.N., Goyal, R.K. Mol. Cell. Biochem. (2003) [Pubmed]
  17. 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. Takishita, E., Takahashi, A., Harada, N., Yamato, M., Yoshizumi, M., Nakaya, Y. J. Cardiovasc. Pharmacol. (2004) [Pubmed]
  18. Impaired potency of bone marrow mononuclear cells for inducing therapeutic angiogenesis in obese diabetic rats. Li, T.S., Furutani, A., Takahashi, M., Ohshima, M., Qin, S.L., Kobayashi, T., Ito, H., Hamano, K. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  19. Anti-mitogenic effects of sarpogrelate in cultured rat mesangial cells. Eto, Y., Nitta, K., Uchida, K., Tsutsui, T., Natori, K., Kawashima, A., Yumura, W., Nihei, H. Life Sci. (1997) [Pubmed]
  20. The effects of sarpogrelate on superoxide production by human neutrophils. Mikawa, K., Akamatsu, H., Nishina, K., Shiga, M., Maekawa, N., Obara, H., Niwa, Y. Regional anesthesia and pain medicine. (2000) [Pubmed]
  21. [2-(O-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding (2). Tanaka, N., Goto, R., Ito, R., Hayakawa, M., Sugidachi, A., Ogawa, T., Asai, F., Fujimoto, K. Chem. Pharm. Bull. (2000) [Pubmed]
  22. Binding and functional affinity of sarpogrelate, its metabolite m-1 and ketanserin for human recombinant alpha-1-adrenoceptor subtypes. Israilova, M., Suzuki, F., Tanaka, T., Nagatomo, T., Taniguchi, T., Muramatsu, I. Pharmacology (2002) [Pubmed]
  23. Effects of sarpogrelate hydrochloride on adenosine diphosphate- or collagen-induced platelet responses in arteriosclerosis obliterans. Nakamura, K., Kariyazono, H., Masuda, H., Sakata, R., Yamada, K. Blood Coagul. Fibrinolysis (2001) [Pubmed]
  24. 5-HT(2) receptor blocker sarpogrelate prevents downregulation of antiapoptotic protein Bcl-2 and protects the heart against ischemia-reperfusion injury. Rajesh, K.G., Suzuki, R., Maeda, H., Murio, Y., Sasaguri, S. Life Sci. (2006) [Pubmed]
  25. Effect of the serotonin blocker sarpogrelate on circulating interleukin-18 levels in patients with diabetes and arteriosclerosis obliterans. Yamakawa, J., Takahashi, T., Saegusa, S., Moriya, J., Itoh, T., Kusaka, K., Kawaura, K., Wang, X.Q., Kanda, T. J. Int. Med. Res. (2004) [Pubmed]
  26. Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Nishio, H., Inoue, A., Nakata, Y. Archives internationales de pharmacodynamie et de thérapie. (1996) [Pubmed]
  27. 5-HT2A receptor subtype in the peripheral branch of sensory fibers is involved in the potentiation of inflammatory pain in rats. Okamoto, K., Imbe, H., Morikawa, Y., Itoh, M., Sekimoto, M., Nemoto, K., Senba, E. Pain (2002) [Pubmed]
  28. Sarpogrelate, a specific 5HT2-receptor antagonist, improves the coronary microcirculation in coronary artery disease. Satomura, K., Takase, B., Hamabe, A., Ashida, K., Hosaka, H., Ohsuzu, F., Kurita, A. Clinical cardiology. (2002) [Pubmed]
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