AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist ( K i of 153 pM), with slightly lesser potency toward 5-HT6 , 5-HT2A , and 5HT-2C receptors ( K i values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 ( K i of 0.58 nM) and adrenergic α2A , α2B , and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis.