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113158-34-2

中文名称 Norbinaltorphimine Dihydrochloride
英文名称 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 结构式 113158-34-2 结构式

基本信息

中文别名
化合物 T12241
英文别名
(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

物理化学性质

熔点>280 °C (decomp)
储存条件Store at RT
溶解度Soluble to 25 mM in water with gentle warming and to 25 mM in DMSO
形态粉末
颜色Light yellow to gray
InChIKeyJOJPJLHRMGPDPV-LZQROVCBSA-N
SMILESCl[H].Cl[H].Oc1ccc2C[C@H]3N(CC[C@@]45[C@@H](Oc1c24)c6[nH]c7[C@@H]8Oc9c(O)ccc%10C[C@H]%11N(CC[C@@]8(c9%10)[C@@]%11(O)Cc7c6C[C@@]35O)CC%12CC%12)CC%13CC%13

安全数据

WGK GermanyWGK 3
存储类别11 - Combustible Solids

常见问题列表

生物活性
Norbinaltorphimine dihydrochloride是一种有效的和选择性的κ阿片受体 (κ opioid receptor) 拮抗剂。
靶点

κ opioid receptor

体外研究

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.

体内研究

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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