Sarpogrelate Hydrochloride 盐酸沙格雷酯

CAS 135159-51-2 MFCD00887582

化学结构图

135159-51-2
SMILES: Cl.COC1C=C(CCC2C=CC=CC=2OCC(CN(C)C)OC(=O)CCC(O)=O)C=CC=1

化学属性

Mol. FormulaC24H31NO6.HCl
Mol. Weight465.97

别名和识别编码

Chemical NameSarpogrelate Hydrochloride
CAS Number135159-51-2
Synonym Butanedioic Acid 1-[2-(Dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl] Anplag Sarpogrelate hydrochloride MCI-9042 Anplag Butanedioic acid 1-[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester hydrochloride MCI 9042 Succinic acid mono-(1-dimethylaminomethyl-2-(2-[2-(3-methoxyphenyl)et hyl]phenoxy)ethyl) ester hydrochloride
MDL NumberMFCD00887582
Chemical Name Translation盐酸沙格雷酯
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分类

  • {SNA} Antagonists, Bioactive Small Molecule Alphabetical Index, Neuroscience, Neurotransmission, Neurotransmitters, S, Serotonergics, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学
  • {SNA} Antagonists, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Neuroscience, Neurotransmission, Neurotransmitters, S, Serotonergics
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • Amines
  • Aromatics

产品应用

  • Sarpogrelate hydrochloride is a potent and selective 5-HT2A receptor antagonist

相关文献及参考

  • [2]. 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.
  • [3]. 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.
  • Skoularigis, J., et al.: Am. J. Cardiol., 71, 587 (1993),
  • [1]. 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.
  • [1]. 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.
  • [2]. Maruyama K, et, al. MCI-9042: high affinity for serotonergic receptors as assessed by radioligand bind

安全信息

Safety Statements
  • S60 This material and its container must be disposed of as hazardous waste 该物质及其容器必须作为危险废物处置;
  • S61 Avoid release to the environment. Refer to special instructions/safety data sheet 避免释放到环境中,参考特别指示/安全收据说明书;
GHS Symbol
WGK Germany3
Precautionary statements
  • P273 Avoid release to the environment. 避免释放到环境中。
Hazard statements
  • H400 Verytoxictoaquaticlife 对水生生物毒性非常大。
  • H302 Harmful if swallowed 吞食有害
Signal word Warning
Hazard Codes Xn,N
Risk Statements
  • R22 Harmful if swallowed 吞咽有害
  • R50/53
RTECSEJ9965500
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 4400 mg/kg
TOXIC EFFECTS :
   Sense Organs and Special Senses (Eye) - effect, not otherwise specified
   Behavioral - somnolence (general depressed activity)
   Behavioral - convulsions or effect on seizure threshold
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 19(Suppl 3),S667,1991

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 108 mg/kg
TOXIC EFFECTS :
   Sense Organs and Special Senses (Eye) - effect, not otherwise specified
   Behavioral - convulsions or effect on seizure threshold
   Gastrointestinal - peritonitis
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 19(Suppl 3),S667,1991

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >3 gm/kg
TOXIC EFFECTS :
   Gastrointestinal - nausea or vomiting
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 19(Suppl 3),S667,1991

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >45 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Ther

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 6240 mg/kg
SEX/DURATION            : female 17-21 day(s) after conception
                          lactating female 21 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Maternal Effects - other effects
   Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
   e.g., stunted fetus)
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 19(Suppl 3),S731,1991

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 27 gm/kg
SEX/DURATION            : male 9 week(s) pre-mating
                          female 2 week(s) pre-mating  - 7 day(s) after
                          conception
TOXIC EFFECTS :
   Reproductive - Maternal Effects - menstrual cycle changes or disorders
   Reproductive - Maternal Effects - other effects
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 19(Suppl 3),S707,1991

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 2080 mg/kg
SEX/DURATION            : female 17-21 day(s) after conception
                          lactating female 21 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4
   per # born alive)
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeuti

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