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AVN-492

CAS No. : 1220646-23-0

MCE 国际站：AVN-492

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: The affinity of AVN-492 to bind to 5-HT6R (K_i=91 pM) is more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (K_i=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.

In Vivo: 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.

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