AVN-492 是一种高特异性的选择性 5-HT6R 拮抗剂，对 5-HT6R 具有皮摩尔级亲和力，K_i 为 91 pM。

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (K i =91 pM).

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5-HT6 Receptor 91 pM (Ki)

The affinity of AVN-492 to bind to 5-HT6R (Ki=91 pM) is more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki=170 nM). Thus, AVN-492 displays great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc. has not independently confirmed the accuracy of these methods. They are for reference only.

In rats, the plasma, brain, and CSF concentrations of the PO administered AVN-492 are dose-dependent. The drug concentration curves for the plasma and brain are of hyperbolic shape and at all doses the brain-plasma ratio is near 11%. The drug concentration in CSF, however, is nearly linearly dependent on the dose, reaching 50% of the plasma level at 10mg/kg. In mice, the plasma and brain concentrations of AVN-492, given IV at a dose of 2 mg/kg, decreased with time but at both time points, 15 min and 60 min, the brain/plasma ratio (mean±SEM) is nearly the same, at 13.2±0.7% and 9.0±1.5%, respectively. This indicates that the steady-state concentration gradient of AVN-492 is established by at least 15 min after the drug administration. has not independently confirmed the accuracy of these methods. They are for reference o

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[1]. Ivachtchenko AV, et al. AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation. J Alzheimers Dis. 2017;58(4):1043-1063.

In Vitro: DMSO : 50 mg/mL (139.10 mM; Need ultrasonic)配制储备液