Y58517 |
Otenzepad |
源叶(MedMol) | 98% |
- 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
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