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189188-57-6

中文名稱 馬來酸替加色羅
英文名稱 Tegaserod maleate
CAS 189188-57-6
分子式 C20H27N5O5
MDL 編號 MFCD04116201
分子量 417.46
MOL 文件 189188-57-6.mol
更新日期 2023/03/20 15:41:21
189188-57-6 結(jié)構(gòu)式 189188-57-6 結(jié)構(gòu)式

基本信息

中文別名
2-[(5-甲氧基-1H-吲哚-3-基)亞甲基]-N-戊基卡巴肼馬來酸鹽
馬來酸替加色羅
替加色羅
英文別名
ELMAC
HTF 919
ZelnorM
Tegibs 6
Toromifene
SDZ-HTF-919
TegaserodMalate
TegastrodMaleate
TEGASEROD MALEATE
Tegaserod Hydrogen Maleate
2-[(5-METHOXY-1H-INDOL-3-YL)METHYLENE]-N-PENTYLHYDRAZINECARBOXIMIDAMIDE, MALEATE
2-[(5-methoxy-1h-indole-3-yl)methylene]-n-pentylcarbazimidamide hydrogen maleate
2-[(5-Methoxy-1H-indol-3-yl)Methylene]-N-pentylhydrazinecarboxiMidaMide (2Z)-2-Butenedioate
SDZ-HTF-919, Zelmac, 2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide, Maleate
所屬類別
原料藥:其它消化系統(tǒng)用藥

物理化學(xué)性質(zhì)

外觀性狀類白色結(jié)晶粉末,熔點(diǎn) 180-183°C
熔點(diǎn)180-183°C
儲存條件2-8°C
溶解度乙腈(微溶、加熱)、DMSO(微溶)、甲醇(微溶)
形態(tài)粉末
顏色白色至米色
CAS 數(shù)據(jù)庫189188-57-6(CAS DataBase Reference)

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS09
警示詞警告
危險(xiǎn)性描述H400-H410-H317

常見問題列表

應(yīng)用
馬來酸替加色羅在臨床應(yīng)用主要是:首先,對IBS 及功能性便秘的治療作用。馬來酸替加色羅是第一個應(yīng)用于治療C -IBS 的5 -HT4受體部分激動劑。
藥理作用
本品是5-HT受體的部分激動劑,與5–HT4受體能緊密結(jié)合,體現(xiàn)高親和力;與5-HT1受體有中度親和力,而對5–HT3受體則不能結(jié)合,體現(xiàn)無親和力。本品激活5-HT4受體可觸發(fā)其他神經(jīng)遞質(zhì)如降鈣素相關(guān)基因肽的釋放,刺激腸蠕動反射及腸道腺體分泌,并抑制內(nèi)臟的敏感性。
毒理研究
在實(shí)驗(yàn)中,動物所用藥物劑量遠(yuǎn)遠(yuǎn)高出了人體臨床治療所推薦劑量。從運(yùn)用該藥及其在人體內(nèi)形成的主要代謝物對兔離體心臟復(fù)極影響的實(shí)驗(yàn)中發(fā)現(xiàn),藥物濃度為0.5 μM 時(shí),Q -T 變化小于5 %;當(dāng)濃度為50μM(人約為人體臨床口服推薦劑量所產(chǎn)生血藥濃度的500 ~1000 倍)時(shí),Q-T 變化為1.4 %。在大鼠、小鼠和狗體中進(jìn)行的高劑量胃腸道影響實(shí)驗(yàn)中,發(fā)現(xiàn)馬來酸替加色羅對相應(yīng)的靶器官無毒性;該薊也不影響免疫系統(tǒng)和生殖能力;在大鼠和小鼠上進(jìn)行的致癌實(shí)驗(yàn)表明該藥也不存在致癌能力,體內(nèi)與體外實(shí)驗(yàn)表明不存在致突變能力,也未使DNA 損害。
生物活性
Tegaserod maleate 是選擇性的、5-HT4 受體的部分激動劑和 5-HT2B 受體的拮抗劑。Tegaserod maleate 在胃腸道中表現(xiàn)出促進(jìn)的作用。
靶點(diǎn)
TargetValue
5-HT4 receptor
()
體外研究

Tegaserod was metabolized in human liver microsomes to O-desmethyl tegaserod at a low rate.
Tegaserod had significant binding affinity for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors (pK i =7.5, 8.4 and 7.0, respectively).
Tegaserod (0.1-3 μM) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA 2 =8.3), consistent with 5-HT2B receptor antagonist activity.

體內(nèi)研究

Tegaserod increases the amplitude of excitatory postsynaptic currents mediated by nicotinic acetylcholine receptors which may contribute to the prokinetic effects by facilitating excitatory neurotransmission in mice.
Tegaserod (0.1 mg/kg) significantly accelerates the gastric emptying rate of glucose in db/db mice, reducing the fraction of the meal remaining in the stomach at 30 min by 80%.
Tegaserod (5, 10, 50, 100 μg/mL) promotes hindlimb motor function at 6 weeks after spinal cord injury compared to the control group receiving vehicle only.

Animal Model: Female C57BLKS/J db/db mice.
Dosage: 0.1, 0.5, 1.0, 2.0 mg/kg.
Administration: IP 15 min prior to gastric loading.
Result: Produced a dramatic decrease in the fraction of the meal remaining in the stomach for doses as low as 0.1 mg/kg (0.1 mg/kg).
Accelerated gastric emptying, with a reduction of nearly 80% in the fraction remaining at 30 min (P < 0.0001) (0.1 mg/kg).
Induced a significant decrease in the gastric emptying rate as the amount of the meal remaining at 30 min was significantly greater (2.0 mg/kg).
Resulted in inhibition of tegaserod-induced increased gastric emptying (0.1 mg/kg).
Animal Model: Three- to four-month-old female C57BL/6J mice.
Dosage: 5, 10, 50, 100 μg/mL.
Administration: Alzet pumps into non-injured spinal cords.
Result: Showed a less intense astrogliosis within and in the vicinity of the compression lesion site when compared to vehicle-only-treated mice.
Showed a smaller lesion area when compared to vehicle-onlytreated mice.
Showed a higher staining intensity of 5-HT-immunoreactive axons 1 mm rostral, but not caudal to the lesion center as determined in cross-sections and quantification by ImageJ analysis.
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