产品描述: PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems |
靶点:
IC50: 4541nM (5-HT3); EC50: 154 nM (α7 nAChR); Ki: 27 nM (R7 MLA);AChR |
体外研究:
PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM. PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM. PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM |
体内研究:
PNU-282987 (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit. PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner. Animal Model: Rats Dosage: 1, 3 mg/kg Administration: i.v. Result: Significantly reversed amphetamine-induced gating deficit. |
参考文献:
1. Alice L Bodnar, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8. |
溶解性:
Soluble in DMSO、H2O |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
3.777 ml |
18.886 ml |
37.771 ml |
5 mM |
0.755 ml |
3.777 ml |
7.554 ml |
10 mM |
0.378 ml |
1.889 ml |
3.777 ml |
50 mM |
0.076 ml |
0.378 ml |
0.755 ml |
|
注意: |
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