AP521

• CAT Number: I020389
• CAS Number: 151227-08-6
• Molecular Formula: C20H19ClN2O3S
• Molecular Weight: 402.89
• Purity: ≥95%
• Synonyms: (3R)-N-(1,3-benzodioxol-5-ylmethyl)-1,2,3,4-tetrahydro-[1]benzothiolo[2,3-c]pyridine-3-carboxamide;hydrochloride
• InChI: InChI=1S/C20H18N2O3S.ClH/c23-20(22-9-12-5-6-16-17(7-12)25-11-24-16)15-8-14-13-3-1-2-4-18(13)26-19(14)10-21-15;/h1-7,15,21H,8-11H2,(H,22,23);1H/t15-;/m1./s1
• InChIKey: IPRJDKMLMDPMBH-XFULWGLBSA-N
• SMILES: C1C(NCC2=C1C3=CC=CC=C3S2)C(=O)NCC4=CC5=C(C=C4)OCO5.Cl

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].

Reference

[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.
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