AVN-101 hydrochloride

AVN-101 hydrochloride 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 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki 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[1].

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

5-HT7 Receptor:0.153 nM (Ki)

5-HT2C Receptor:1.17 nM (Ki)

5-HT2A Receptor:1.56 nM (Ki)

5-HT6 Receptor:2.04 nM (Ki)

5-HT2B Receptor:10.6 nM (Ki)

5-HT1A Receptor:61 nM (Ki)

5-HT1B Receptor:720 nM (Ki)

H1 Receptor:0.58 nM (Ki)

Alpha-2B adrenergic receptor:0.41 nM (Ki)

Alpha-2A adrenergic receptor:1.77 nM (Ki)

Alpha-2C adrenergic receptor:3.55 nM (Ki)

Alpha-1B adrenergic receptor:9.4 nM (Ki)

Alpha-1A adrenergic receptor:18.9 nM (Ki)

Alpha-1D adrenergic receptor:30.2 nM (Ki)

[1]. Alexandre V Ivachtchenko, et al. AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. J Alzheimers Dis. 2016 May 25;53(2):583-620.