产品
编 号:F238878
分子式:C13H20ClNOS
分子量:273.82
产品类型
结构图
CAS No: 191611-89-9
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产品详情
生物活性:
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
体内研究:
SIB-1553A (1-40 mg/kg; s.c.) produces dose-dependent increases in ACh levels.Animal Model:Male Sprague-Dawley rats (200-250 g)
Dosage:1, 2, 4, 10, 20 and 40 mg/kg
Administration:s.c.
Result:Induced hippocampal ACh release.
体外研究:
SIB-1553A displaces the binding of [H]nicotine (NIC) to the rat brain nAChRs with an IC50 value of 110 nM.In calcium flux assays, SIB-1553A (0.1-5 μM), shows a greater selectivity for beta4-subunit containing recombinant hnAChRs (alpha2beta4, alpha3beta4 and alpha4beta4) vs. beta2-subunit containing nAChRs (alpha4beta2 and alpha3beta2) both in terms of efficacy and potency.