AR-A 2

AR-A 2 is a selective 5-HT_1B receptor antagonist, with high affinity to guinea pig cortex 5HT_1B/1D and recombinant guinea pig 5-HT_1B receptors (K_i=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT_1D receptor (K_i, 5 nM), and shows an EC₅₀ of 4.5 nM for the guinea pig 5-HT_1B receptor; AR-A 2 can be used in the research of depression and anxiety. IC50 & Target: EC50: 4.5 nM (guinea pig 5-HT_1B receptor)^[1]
Ki: 0.24 nM (guinea pig cortex 5HT_1B/1D), 0.47 nM (recombinant guinea pig 5-HT_1B receptor), 5 nM (guinea pig 5-HT_1D receptor), 20 nM (rat cortical 5HT_1B/1D receptor), 339 nM (rat cortex 5-HT_2A receptor), 3070 nM (Rat hippocampus 5-HT_1A receptor), 330 nM (dopamine D2), 490 nM (α1-adrenoceptor)^[1] In Vitro: AR-A 2 (AR-A000002) is a selective 5-HT_1B receptor antagonist, with high affinity to guinea pig cortex 5HT_1B/1D and recombinant guinea pig 5-HT_1B receptors (K_i=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT_1D receptors (K_i, 5 nM), and shows an EC₅₀ of 4.5 nM for the guinea pig 5-HT_1B receptor. AR-A 2 also binds to the rat cortical 5HT_1B/1D receptor (K_i, 20 nM), rat cortex 5-HT_2A receptor (K_i, 339 nM), rat hippocampus 5-HT_1A receptor (K_i, 3070 nM). In addition, AR-A 2 also exhibits affinity for dopamine D2 (K_i, 330 nM) and α1-adrenoceptors (K_i, 490 nM)^[1].