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

基本信息物理化学性质常见问题列表

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

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.