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1216621-00-9

中文名稱 1-(1-(cyclooctylMethyl)-5-(hydroxyMethyl)-1,2,3,6-tetrahydropyridin-4-yl)-3-ethyl-1H-benzo[d]iMidazol-2(3H)-one hydrochloride
英文名稱 1-(1-(cyclooctylMethyl)-5-(hydroxyMethyl)-1,2,3,6-tetrahydropyridin-4-yl)-3-ethyl-1H-benzo[d]iMidazol-2(3H)-one hydrochloride
CAS 1216621-00-9
分子式 C24H36ClN3O2
分子量 434.015
MOL 文件 1216621-00-9.mol
1216621-00-9 結(jié)構(gòu)式 1216621-00-9 結(jié)構(gòu)式

基本信息

中文別名
化合物 T23475
TRAP-101鹽酸鹽
英文別名
Trap-101 hydrochloride
Trap-101 hydrochloride >=98% (HPLC), powder
1-[1-(cyclooctylmethyl)-5-(hydroxymethyl)-3,6-dihydro-2H-pyridin-4-yl]-3-ethylbenzimidazol-2-one:hydrochloride
1-(1-(cyclooctylMethyl)-5-(hydroxyMethyl)-1,2,3,6-tetrahydropyridin-4-yl)-3-ethyl-1H-benzo[d]iMidazol-2(3H)-one hydrochloride

物理化學(xué)性質(zhì)

儲(chǔ)存條件2-8°C
溶解度H2O:≥10mg/mL
形態(tài)粉末
顏色白色至灰白色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301
防范說明P301+P310
危險(xiǎn)品標(biāo)志T
危險(xiǎn)類別碼25
安全說明45
危險(xiǎn)品運(yùn)輸編號(hào)UN 2811 6.1 / PGIII
WGK Germany3

常見問題列表

生物活性
Trap-101 hydrochloride 是一種有效的,選擇性和競(jìng)爭(zhēng)性的 NOP receptors 拮抗劑 ,對(duì) NOP 受體的選擇性高于對(duì)其他的阿片受體。Trap-101 刺激 GTPγ35S 結(jié)合到 CHOhNOP,NOP、μ-,κ- 和 δ 阿片受體的 pKi 值分別為 8.65, 6.60, 6.14 和 <5。Trap-101 減弱帕金森病大鼠運(yùn)動(dòng)缺陷,可用于神經(jīng)系統(tǒng)疾病的研究。
靶點(diǎn)

pKi: 8.65 (NOP receptor); 6.60 (μ-opioid receptor); 6.14 (κ-opioid receptor); < 5?(δ-opioid receptor)

體外研究

Trap-101 hydrochloride (3, 30, and 300 nM) is inactive per se up to 10 μM, while in the range 3-300 nM, it produces a concentration dependent rightward shift of the concentration-response curve to N/OFQ without modifications of the maximal response to the agonist. Receptor binding affinities of Trap101 (pK i values) at recombinant human NOP, and classical opioid receptors expressed in CHO cell membranes are 8.65, 6.60, 6.14 and < 5 for NOP,?μ-,?κ-, and?δ-opioid receptors respectively.

體內(nèi)研究

Trap-101 hydrochloride (10-30 mg/kg; detected after 90 min) changes motor activity in na?ve rats, it causes a delayed increase in the immobility time in the bar test at 30 mg/kg, Moreover, it increased stepping activity and rotarod performance at 10 mg/kg and reduces them at 30 mg/kg.6-OHDA lesioning produces motor asymmetry mostly affecting the contralateral paw and overall reduced motor performance. Trap-101 hydrochloride (intraperitoneal?injection; 10-30 mg/kg; detected after 90 min) alleviates akinesia/bradykinesia and improves overall gait ability in hemiparkinsonian rats, being effective starting at 1 mg/kg and without worsening motor deficit at 30 mg/kg.

Animal Model: 6-OHDA hemilesioned rats
Dosage: 10-30 mg/kg
Administration: Intraperitoneal?injection; 10-30 mg/kg; detected after 90 min
Result: Attenuated parkinsonian-like motor deficits in rat.
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