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AS 19
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AS 19图片
CAS NO:1000578-26-6
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
AS 19 是一种有效的选择性 5-HT7 受体激动剂，IC50 值为 0.83 nM，Ki 值为 0.6 nM。
Cas No.1000578-26-6
化学名(2S)-N,N-dimethyl-8-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1,2,3,4-tetrahydronaphthalen-2-amine
Canonical SMILESCC1=NN(C(C)=C1C2=CC=CC3=C2C[C@](N(C)C)([H])CC3)C
分子式C18H25N3
分子量283.41
溶解度<28.34mg/ml in ethanol;<28.34mg/ml in DMSO
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AS 19 is a potential 5-HT7 receptor agonist with an IC50 value of 0.83 nM [1].

5-HT7 receptor plays a role in the control of both sleep and circadian rhythms. This receptor may also play a role in other CNS disorders including cognitive disturbances, anxiety and migraine probably via both central and peripheral mechanisms [2].

By signaling through the 5-HT7 receptor, serotonin provides an accessory signal to enhance the activation of the T-cell. Compared with saline-treated controls, the proliferation of T-cell from PCPA-treated mice was significantly reduced. The PCPA inhibition efficacy ranged from approximately 18% to 49%. Addition of exogenous 5-HT at 1 μM completely restored the proliferation of the T-cell. Similar to exogenous 5-HT, addition of AS19 at 1 μM also completely restored T-cell proliferation after 48 hours [4].

SB-258719 is a selective 5-HT7 receptor antagonist. When AS-19 at a dose of 10 mg/kg was co-administered with SB-258719 at the same dose, which produced no effect on its own, the anti-hyperalgesic effect of AS-19 was reversed in both hotplate and tail-flick tests. That meant AS-19 exerts anti-hyperalgesic effect via 5-HT7 receptors [3]. SB269970 is also a selective 5-HT7 receptor antagonist. Some rats were prepared with a second intrathecal catheter and were pretreated with 7μl SB269970 at a concentration of 5mM. At all time points, AS-19-induced PMF was abolished by SB269970 pretreatment. This meant AS-19 elicited PMF via the activation of 5-HT7 receptor [5].

References:
[1].  Perez-García GS and Meneses A. Effects of the potential 5-HT7 receptor agonist AS 19 in an autoshaping learning task. Behav Brain Res, 2005, 163(1):136-40.
[2].  Thomas DR and Hagan JJ. 5-HT7 Receptors. Current Drug Targets-CNS & Neurological Disorders, 2004, 3(1): 81-90.
[3].  Ulugol A, Oltulu C, Gunduz O, et al. 5-HT7 receptor activation attenuates thermal hyperalgesia in streptozocin-induced diabetic mice. Pharmacol Biochem Behav, 2012, 102(2):344-8.
[4].  León-Ponte M, Ahern GP and O'Connell PJ. Serotonin provides an accessory signal to enhance T-cell activation by signaling through the 5-HT7 receptor. Blood, 2007, 109(8):3139-46.
[5].  Hoffman MS and Mitchell GS. Spinal 5-HT7 receptor activation induces long-lasting phrenic motor facilitation. J Physiol, 2011, 589(Pt 6):1397-407.