AP521
- Product Name
- AP521
- CAS No.
- 151227-08-6
- Chemical Name
- AP521
- Synonyms
- AP521;AP521,AP-521;N-(1,3-Benzodioxol-5-ylmethyl)-1,2,3,4-tetrahydro-[1]benzothiolo[2,3-c]pyridine-3-carboxamide hydrochloride
- CBNumber
- CB74796632
- Molecular Formula
- C20H19ClN2O3S
- Formula Weight
- 402.89
- MOL File
- 151227-08-6.mol
AP521 Property
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CCH0007832
- Product name
- (4R)-N-(2H-1,3-BENZODIOXOL-5-YLMETHYL)-8-THIA-5-AZATRICYCLO[7.4.0.0(2,7)]TRIDECA-1(9),2(7),10,12-TETRAENE-4-CARBOXAMIDE HYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $503.47
- Updated
- 2021/12/16
AP521 Chemical Properties,Usage,Production
Uses
AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
in vivo
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].
IC 50
5-HT1A Receptor: 94 nM (IC50, in human); 5-HT1A Receptor: 135 nM (IC50, in rat); 5-HT1B Receptor: 254 nM (IC50, in rat); 5-HT1B Receptor: 5530 nM (IC50, in human); 5-HT1D Receptor: 418 nM (IC50, in human); 5-HT5A Receptor: 422 nM (IC50, in human); 5-HT7 Receptor: 198 nM (IC50, in rat)
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. DOI:10.1016/j.jphs.2014.11.008
AP521 Preparation Products And Raw materials
Raw materials
Preparation Products
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