AP521 |
| رقم الكتالوجGC31134 |
AP521 هو ناهض لمستقبلات الإنسان 5-HT1A مع IC50 من 94 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 151227-08-6
Sample solution is provided at 25 µL, 10mM.
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AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
AP521 is an agonist of human 5-HT1A receptor with IC50s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT1A (rat), 5-HT1A (human), 5-HT1B (rat), 5-HT1B (human), 5-HT1D (human), 5-HT5a (human) and 5-HT7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM[1].
AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant[1].
[1]. Kasahara K, et al. The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats. J Pharmacol Sci. 2015 Jan;127(1):109-16.
Cell experiment: | in vitro studies, AP521 is dissolved with DMSO.--> Membranes of neurotransmitter receptors are prepared from the tissues of rat, mouse, and guinea pig or from recombinant cells. These membranes are incubated in assay buffers containing selective radioligand for each receptor and AP521. After the incubation, the mixture is vacuum filtered through a glass membrane filter and washed by cold reaction buffer. Afterward, the radioactivity of the filters is counted[1]. |
Animal experiment: | Male Sprague-Dawley rats weighing 250 to 300 g are anesthetized with pentobarbital sodium (50 mg/kg, i.p.) and placed on a stereotaxic apparatus. Dialysis probes with an outer diameter of 0.105 mm are inserted into the guide cannulae so that 3.0 mm of the probes are exposed to the tissue of the medial prefrontal cortex. Rats are housed individually after these operations. On the following day, perfusion is started in the home cage using artificial cerebrospinal fluid (145 mM NaCl, 3.0 mM KCl, 1.3 mM CaCl2, 1.0 mM MgCl2) at a flow rate of 2 mL/min. AP521 (3, 10 mg/kg), tandospirone (10 mg/kg) or vehicle are administered subcutaneously 60 min after sample collection started. The dialysate samples are collected every 30 min for 180 min and extracellular levels of 5-HT are determined[1]. |
References: [1]. Kasahara K, et al. The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats. J Pharmacol Sci. 2015 Jan;127(1):109-16. | |
| Cas No. | 151227-08-6 | SDF | |
| Canonical SMILES | O=C([C@H]1CC(C2=CC=CC=C2S3)=C3CN1)NCC4=CC=C(OCO5)C5=C4.[H]Cl | ||
| Formula | C20H19ClN2O3S | M.Wt | 402.89 |
| الذوبان | Soluble in DMSO | Storage | Store 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. |
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| 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 | 2.4821 mL | 12.4103 mL | 24.8207 mL |
| 5 mM | 0.4964 mL | 2.4821 mL | 4.9641 mL |
| 10 mM | 0.2482 mL | 1.241 mL | 2.4821 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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