WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555161
Description: AVN-492 is a potent and selective 5-HT6R Antagonist. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). AVN-492 demonstrates good in vitro and in vivo ADME profile with high oral bioavailability and good brain permeability in rodents.
MedKoo Cat#: 555161
Chemical Formula: C17H21N5O2S
Exact Mass: 359.1416
Molecular Weight: 359.448
Elemental Analysis: C, 56.81; H, 5.89; N, 19.48; O, 8.90; S, 8.92
Synonym: AVN-492; AVN 492; AVN492.
IUPAC/Chemical Name: N2,N6,N6,5,7-pentamethyl-3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine-2,6-diamine
InChi Key: SNPPEHMSSOEYDH-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H21N5O2S/c1-11-14(21(4)5)12(2)22-17(19-11)15(16(18-3)20-22)25(23,24)13-9-7-6-8-10-13/h6-10H,1-5H3,(H,18,20)
SMILES Code: CNC1=NN2C(N=C(C)C(N(C)C)=C2C)=C1S(C3=CC=CC=C3)(=O)=O
In behavioral tests, AVN-492 shows anxiolytic effect in elevated plus-maze model, prevents an apomorphine-induced disruption of startle pre-pulse inhibition (the PPI model) and reverses a scopolamine- and MK-801-induced memory deficit in passive avoidance model. No anti-obesity effect of AVN-492 was found in a murine model. The data presented here strongly indicate that due to its high oral bioavailability, extremely high selectivity, and potency to block the 5-HT6 receptor, AVN-492 is a very promising tool for evaluating the role the 5-HT6 receptor might play in cognitive and neurodegenerative impairments. AVN-492 is an excellent drug candidate to be tested for treatment of such diseases, and is currently being tested in Phase I trials.
1: Ivachtchenko AV, Okun I, Aladinskiy V, Ivanenkov Y, Koryakova A, Karapetyan R,
Mitkin O, Salimov R, Ivashchenko A. AVN-492, A Novel Highly Selective 5-HT6R
Antagonist: Preclinical Evaluation. J Alzheimers Dis. 2017;58(4):1043-1063. doi:
10.3233/JAD-161262. PubMed PMID: 28550249.