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113158-34-2

中文名稱 Norbinaltorphimine Dihydrochloride
英文名稱 Norbinaltorphimine Dihydrochloride
CAS 113158-34-2
分子式 C40H43N3O6.2HCl
分子量 698.26
MOL 文件 113158-34-2.mol
113158-34-2 結(jié)構(gòu)式 113158-34-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12241
英文別名
(1S,2S,7S,8S,12R,20R,24R,32R)-11,33-bis(cyclopropylmethyl)-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaene-2,7,17,27-tetrol

物理化學(xué)性質(zhì)

熔點(diǎn)>280 °C (decomp)
儲(chǔ)存條件Store at RT
溶解度Soluble to 25 mM in water with gentle warming and to 25 mM in DMSO
形態(tài)粉末
顏色Light yellow to gray

常見問題列表

生物活性
Norbinaltorphimine dihydrochloride是一種有效的和選擇性的κ阿片受體 (κ opioid receptor) 拮抗劑。
靶點(diǎn)

κ opioid receptor

體外研究

Norbinaltorphimine reversibly antagonize the effects of κ agonists with pA2 values of 10.2-10.4. Norbinaltorphimine is much less potent as an antagonist at μ and δ receptors, pA2 values are 7.4-7.6 and 7.6-7.8, respectively.

體內(nèi)研究

Norbinaltorphimine has weak and inconsistent effects on THC-induced taste avoidance in adolescent rats in that Norbinaltorphimine both attenuates and strengthens taste avoidance dependent on dose and trial. Norbinaltorphimine has limited impact on the final one-bottle avoidance and no effects on the two-bottle preference test. Interestingly, Norbinaltorphimine has no effect on THC-induced taste avoidance in adult rats as well. Norbinaltorphimine pretreatment significantly attenuates stress-induced reinstatement of nicotine-CPP, but has no effect on nicotine-primed reinstatement.

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