AVN-101

Uses

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].

IC 50

5-HT₇ Receptor: 0.153 nM (Ki); 5-HT_2C Receptor: 1.17 nM (Ki); 5-HT_2A Receptor: 1.56 nM (Ki); 5-HT₆ Receptor: 2.04 nM (Ki); 5-HT_2B Receptor: 10.6 nM (Ki); 5-HT_1A Receptor: 61 nM (Ki); 5-HT_1B 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)

References

[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. DOI:10.3233/JAD-151146