产品
编 号:F332097
分子式:C27H31Cl2N5O3
分子量:544.47
产品类型
结构图
CAS No: 351183-88-5
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产品详情
生物活性:
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor.
体内研究:
5'-Guanidinonaltrindole (5'-GNTI) (0.03-3 mg/kg; s.c.; once) induces scratching in mice.Animal Model:Male Swiss-Webster mice
Dosage:0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:Subcutaneous injection, once
Result:Induced scratching, the scratch A50 value was calculated to be 0.17 mg/kg.
体外研究:
5'-Guanidinonaltrindole (5'-GNTI) also binds to human μ- and δ-opioid receptors with Kis of 36.9±2.3 nM and 70.0±0.3 nM, respectively.5'-Guanidinonaltrindole is most effective at κ-opioid receptors (pA2=10.4±0.10), with substantially lower antagonist potency at μ-opioid (pA2=8.49±0.09) and δ-opioid receptors (pA2=7.81±0.06).