AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic alpha2A, alpha2B, and alpha2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimers disease, and multiple sclerosis[1].
