AS 19 |
| رقم الكتالوجGC17525 |
AS 19 هو ناهض مستقبلات 5-HT7 انتقائي قوي بقيمة IC50 تبلغ 0.83 نانومتر و Ki يبلغ 0.6 نانومتر.
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Cas No.: 1000578-26-6
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1000578-26-6 | SDF | |
| Chemical Name | (2S)-N,N-dimethyl-8-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1,2,3,4-tetrahydronaphthalen-2-amine | ||
| Canonical SMILES | CC1=NN(C(C)=C1C2=CC=CC3=C2C[C@](N(C)C)([H])CC3)C | ||
| Formula | C18H25N3 | M.Wt | 283.41 |
| الذوبان | <28.34mg/ml in ethanol; <28.34mg/ml in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5285 mL | 17.6423 mL | 35.2846 mL |
| 5 mM | 0.7057 mL | 3.5285 mL | 7.0569 mL |
| 10 mM | 0.3528 mL | 1.7642 mL | 3.5285 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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