사포그렐라목

Sarpogrelate
사포그렐라목
Sarpogrelate structure.png
임상자료
기타 이름사르포그렐레이트(----4-[1-디메틸아미노-3-[2-[2-(3-메톡시페닐)에틸]페녹시]프로판-2-yl]옥시-4-옥소부타노산
AHFS/Drugs.com국제 마약 이름
ATC 코드
  • 없는
식별자
  • 4-[2-(dimethylamino)-1-({2-[2-(3-메톡시페닐)ethyl]phenoxy}메틸)ethoxy]-4-oxobutanoic acid
CAS 번호
펍켐 CID
IUPHAR/BPS
켐스파이더
유니
켐벨
CompTox 대시보드 (EPA)
화학 및 물리적 데이터
공식C24H31NO6
어금질량429.513 g·1998−1
3D 모델(JSmol)
  • CN(C)CC(COC1=CC=CC1CC2=CC(=CC=C2)OC)OC(=O)CC(=O)o
  • InChI=1S/C24H31NO6/c1-25(2)16-21(31-24(28)14-13-23(26)27)17-30-22-10-5-4-8-19(22)12-11-18-7-6-9-20(15-18)29-3/h4-10,15,21H,11-14,16-17H2,1-3H3,(H,26,27) ☒N
  • 키:FFINAVGJSYHFO-UHFFFAOYSA-N ☒N
☒NcheckY (이게 뭐야?) (iii)

사르포그렐레이트(이전의 개발코드명 MCI-9042, LS-187,118)는 5HT2A[1][2] 수용체와 5HT2B[3] 수용체에서 길항제 역할을 하는 약물이다. 세로토닌 유도 혈소판 집적을 차단하고, 당뇨병, [4][5]부에거병,[6] 레이노우드병, 관상동맥질환,[7][8] 협심증,[9] 동맥경화증 등 많은 질병의 치료에 응용이 가능하다.[10]

참고 항목

참조

  1. ^ Pertz H, Elz S (April 1995). "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". The Journal of Pharmacy and Pharmacology. 47 (4): 310–6. doi:10.1111/j.2042-7158.1995.tb05801.x. PMID 7791029. S2CID 25311518.
  2. ^ Nishio H, Inoue A, Nakata Y (1996). "Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes". Archives Internationales de Pharmacodynamie et de Therapie. 331 (2): 189–202. PMID 8937629.
  3. ^ Muntasir HA, Hossain M, Bhuiyan MA, Komiyama T, Nakamura T, Ozaki M, Nagatomo T (July 2007). "Identification of a key amino acid of the human 5-HT(2B) serotonin receptor important for sarpogrelate binding". Journal of Pharmacological Sciences. 104 (3): 274–7. doi:10.1254/jphs.sc0060241. PMID 17609583.
  4. ^ Pietraszek MH, Takada Y, Taminato A, Yoshimi T, Watanabe I, Takada A (April 1993). "The effect of MCI-9042 on serotonin-induced platelet aggregation in type 2 diabetes mellitus". Thrombosis Research. 70 (2): 131–8. doi:10.1016/0049-3848(93)90154-g. PMID 8322284.
  5. ^ Ogawa S, Takeuchi K, Sugimura K, Sato C, Fukuda M, Lee R, et al. (1999). "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". Clinical and Experimental Pharmacology & Physiology. 26 (5–6): 461–4. doi:10.1111/j.1440-1681.1999.03056.x. PMID 10386239. S2CID 31041268.
  6. ^ Rydzewski A, Urano T, Hachiya T, Kaneko H, Baba S, Takada Y, Takada A (December 1996). "The effect of a 5HT2 receptor antagonist sarpogrelate (MCI-9042) treatment on platelet function in Buerger's disease". Thrombosis Research. 84 (6): 445–52. doi:10.1016/s0049-3848(96)00212-5. PMID 8987165.
  7. ^ Igarashi M, Okuda T, Oh-i T, Koga M (October 2000). "Changes in plasma serotonin concentration and acceleration plethysmograms in patients with Raynaud's phenomenon after long-term treatment with a 5-HT2 receptor antagonist". The Journal of Dermatology. 27 (10): 643–50. doi:10.1111/j.1346-8138.2000.tb02246.x. PMID 11092268. S2CID 24884976.
  8. ^ Satomura K, Takase B, Hamabe A, Ashida K, Hosaka H, Ohsuzu F, Kurita A (January 2002). "Sarpogrelate, a specific 5HT2-receptor antagonist, improves the coronary microcirculation in coronary artery disease". Clinical Cardiology. 25 (1): 28–32. doi:10.1002/clc.4950250108. PMC 6654074. PMID 11808836.
  9. ^ Kinugawa T, Fujita M, Lee JD, Nakajima H, Hanada H, Miyamoto S (August 2002). "Effectiveness of a novel serotonin blocker, sarpogrelate, for patients with angina pectoris". American Heart Journal. 144 (2): A1–A6. doi:10.1067/mhj.2002.124056. PMID 12177659.
  10. ^ Hayashi T, Sumi D, Matsui-Hirai H, Fukatsu A, Arockia Rani PJ, Kano H, et al. (May 2003). "Sarpogrelate HCl, a selective 5-HT2A antagonist, retards the progression of atherosclerosis through a novel mechanism". Atherosclerosis. 168 (1): 23–31. doi:10.1016/s0021-9150(03)00054-6. PMID 12732383.