AVN-492

AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM). It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.Formal Name: N2,N6,N6,5,7-pentamethyl-3-(phenylsulfonyl)-pyrazolo[1,5-a]pyrimidine-2,6-diamine. CAS Number: 1220646-23-0. Molecular Formula: C17H21N5O2S. Formula Weight: 359.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:20): 0.04 mg/ml, DMSO: 25 mg/ml, Ethanol: 1 mg/ml. lambdamax: 247 nm. SMILES: CN(C)C(C(C)=N1)=C(C)N2C1=C(S(C3=CC=CC=C3)(=O)=O)C(NC)=N2. InChi Code: InChI=1S/C17H21N5O2S/c1-11-14(21(4)5)12(2)22-17(19-11)15(16(18-3)20-22)25(23,24)13-9-7-6-8-10-13/h6-10H,1-5H3,(H,18,20). InChi Key: SNPPEHMSSOEYDH-UHFFFAOYSA-N.