AVN-492

SKU: orb1302022

Description

AVN-49 is a highly potent and selective serotonin 5-HT6 receptor antagonist with a Ki value of 91 pM. This compound is a valuable research tool for investigating the role of the 5-HT6 receptor in neuropsychiatric disorders, including cognitive deficits, in both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1220646-23-0
• MW: 359.45
• Purity: 99.29%
• Formula: C₁₇H₂₁N₅O₂S
• SMILES: CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1
• Target: 5-HT Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.78 mM);DMSO:7.5 mg/mL (20.87 mM)

Bioactivity

• Target IC50:
  5-HT6 receptor:91 pM (Ki, cell free)
• In Vivo:
  AVN-492 has high oral bioavailability and good brain permeability in rodents. In behavioral tests, AVN-492 shows an anxiolytic effect in the elevated plus-maze model, prevents an apomorphine-induced disruption of startle pre-pulse inhibition (the PPI model) and reverses scopolamine- and MK-801-induced memory deficit in passive avoidance model. No anti-obesity effect of AVN-492 was found in a murine model .
• In Vitro:
  Affinity of AVN-492, Ki^b, to compete with [3H]LSD for binding to 5-HT6R was estimated to be 91 pM (IC50^b = 194 pM). Affinity of 509 AVN-492 to the 5-HT2BR, Ki^b = 170 nM (IC50^b = 268 nM) was more than three orders of magnitude lower. Despite being metabolized by human microsomes, AVN-492 did not appreciably inhibit five major human recombinant CYP isoforms, CYP3A4, 1A2, 2C9, 2C19, and 2D6 at concentrations as high as 10 M .
• Animal Research:
  For pharmacokinetic, behavior, and toxicity studies, male Wistar rats (220–242 g), male CD1 mice (24–30 g), male SHK mice (20–25 g), and male Balb/C mice (15–20 g) were used. Rodents were obtained from Jackson Laboratories and housed in a standard laboratory animal facility in groups of 5–7 animals per cage. Before entering the investigation, the animals were acclimated at least for seven days. Obese C57BL/6 male 18-week-old mice were obtained from Jackson Laboratories. The mice were fed on a high-fat diet (60% kcal Research Diet 12492i) from the age of 6 weeks. Upon arrival, the mice were maintained on the same high fat diet with free access to both food and water. The mice were individually housed in solid bottom static isolators with Bed-O'Cobs bedding inside a BioBUBBLE clean room that provided HEPA-filtered air into the clean room environment at a rate of 100 complete air changes per hour. All treatments and procedures including body weight determinations, drug administration, and glucose measurements were carried out in the clean room environment .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AVN 492, AVN492, AVN-492, 5HT Receptor, 5-HT Receptor, 5-HT6, 5-hydroxytryptamine Receptor, 5HTReceptor, inhibit, Inhibitor, Serotonin Receptor

Compound Identifiers

PubChem CID

56655571