Sarpogrelate Hydrochloride 盐酸沙格雷酯
CAS 135159-51-2 MFCD00887582
化学结构图
SMILES: Cl.COC1C=C(CCC2C=CC=CC=2OCC(CN(C)C)OC(=O)CCC(O)=O)C=CC=1
化学属性
| Mol. Formula | C24H31NO6.HCl |
|---|---|
| Mol. Weight | 465.97 |
别名和识别编码
| Chemical Name | Sarpogrelate Hydrochloride |
|---|---|
| CAS Number | 135159-51-2 |
| 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 Number | MFCD00887582 |
| 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
- 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
- P273 Avoid release to the environment. 避免释放到环境中。
- H400 Verytoxictoaquaticlife 对水生生物毒性非常大。
- H302 Harmful if swallowed 吞食有害
- R22 Harmful if swallowed 吞咽有害
- R50/53
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),S731,1991TYPE 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),S707,1991TYPE 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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