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99755-59-6

中文名稱(chēng) 羅替戈汀
英文名稱(chēng) ROTIGOTINE
CAS 99755-59-6
分子式 C19H25NOS
分子量 315.47
MOL 文件 99755-59-6.mol
更新日期 2024/10/30 22:19:55
99755-59-6 結(jié)構(gòu)式 99755-59-6 結(jié)構(gòu)式

基本信息

中文別名
羅替戈汀
羅替戈汀堿
羅替戈汀雜質(zhì)
羅替哥汀雜質(zhì)
羅替戈汀 100MG
ROTIGOTINE(S構(gòu)型)
(S)-5,6,7,8-四氫-6-(丙基(2-(2-噻吩基)乙基)氨基)-1-萘酚
英文別名
CS-110
Neupro
N 0923
SPM 962
Rotigotine
S(-)-N-0437
Rotigotine (Base)
ROTIGOTINE USP/EP/BP
(S)-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol
[S,(-)]-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol
所屬類(lèi)別
生物化工:Dopamine Receptor 激動(dòng)劑

物理化學(xué)性質(zhì)

熔點(diǎn)78 °C
沸點(diǎn)470.1±45.0 °C(Predicted)
密度1.15±0.1 g/cm3(Predicted)
儲(chǔ)存條件room temp
溶解度DMF: 30 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml; DMSO: 20 mg/ml; Ethanol: 1 mg/ml
水溶解性不溶于水
酸度系數(shù)(pKa)10.49±0.40(Predicted)
形態(tài)粉末晶體
顏色白色到近乎白色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS08
警示詞警告
危險(xiǎn)性描述H336-H362-H361
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類(lèi)別碼22
海關(guān)編碼2934990002
毒害物質(zhì)數(shù)據(jù)99755-59-6(Hazardous Substances Data)

常見(jiàn)問(wèn)題列表

生物活性
Rotigotine是一種dopamine receptor的激動(dòng)劑,用于帕金森氏癥和不寧腿綜合征的治療。
靶點(diǎn)
TargetValue
Dopamine receptor
體外研究

Rotigotine (N-0437; N-0923) has a 10-fold selectivity for D3 (pK i 9.2) receptors compared with D2, D4 and D5 (pK i 8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK i 7.2). In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC 50 respectively: 9.0, 9.4-8.6, 9.7).
Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 μM) slightly protects dopaminergic neurons against MPP + toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.

體內(nèi)研究

In primed rats, Rotigotine (N-0437; N-0923; 0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.

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