产品描述: | Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively |
靶点: |
640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart);AChR |
体外研究: |
Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls. Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls. Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory. |
体内研究: |
Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls. Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls. Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory. Animal Model: Forty-eight male Long-Evans rats (325-350 g). Dosage: 0.25, 0.5, 1.0 and 2.0 mg/kg. Administration: S.C. on the dorsum of the neck once. Result: Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect. Animal Model: Adult male Swiss mice (age 60–70 days; weight 25-30 g). Dosage: 0.3, 1.0, or 3.0 mg/kg. Administration: IP once. Result: Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U15,15 = 49, p < 0.02, compared with saline-saline-injected control group). |
参考文献: |
1. Bloom JW, et al. Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116. Life Sci. 1987 Jul 27;41(4):491-6. 2. Packard MG, et al. Post-training injection of the acetylcholine M2 receptor antagonist AF-DX 116 improves memory. Brain Res. 1990 Jul 30;524(1):72-6. 3. Kopf SR, et al. AF-DX 116, a presynaptic muscarinic receptor antagonist, potentiates the effects of glucose and reverses the effects of insulin on memory. Neurobiol Learn Mem. 1998 Nov;70(3):305-13. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.372 ml |
11.861 ml |
23.723 ml |
5 mM |
0.474 ml |
2.372 ml |
4.745 ml |
10 mM |
0.237 ml |
1.186 ml |
2.372 ml |
50 mM |
0.047 ml |
0.237 ml |
0.474 ml |
|
注意: |
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