货号 | 5112/50 |
别名 | 3-[3-(3-Pyridinyl)-1,2,4-oxadiazol- |
供应商 | Tocris |
生物活性 | Positive allosteric modulator of α4β2 receptor; increases the potency of Ach-evoked currents ~60 fold without effecting the maximum efficacy (HEK293-hα4β2 cells). Reduces the rate of recovery from desensitization and slows the rate of deactivation. Displays a synergistic effect on the Emax when given with NS206 at 3α:2βreceptors. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 248.24 |
分子式 | C14H8N4O |
可溶性/溶解性 | Soluble to 50 mM in DMSO and to 20 mM in 1eq. HCl |
参考文献 | Mohleret al (2014) Discriminative-stimulus effects of NS9283, a nicotinic α4β2* positive allosteric modulator, in nicotine-discriminating rats. Psychopharmacology (Berl). 231 67. PMID: 23925734. Grupeet al (2013) Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. Br.J.Pharmacol. 168 2000. PMID: 23278456. Olsenet al (2013) Two distinct allosteric binding sites at α4β2 nicotinic acetylcholine receptors revealed by NS206 and NS9283 give unique insights to binding activity-associated linkage at Cys-loop receptors. J.Biol.Chem. 288 35997. PMID: 24169695. |