AVN492

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AVN-492 是一种有效的选择性 5-HT6R 拮抗剂 (Ki: 91 pM)。

AVN-492 is a potent and selective 5-HT6R Antagonist (Ki:?91 pM).

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.

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.

——

Endocrinology/Hormones

5-HT Receptor

5-HT6|5-HT6R

——

——

1220646-23-0

359.45

C17H21N5O2S

>98% (HPLC)

DMSO: 100 mg/mL

CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1

N2N6N657-pentamethyl-3-(phenylsulfonyl)pyrazolo[15-a]pyrimidine-26-diamine

(-20℃)

With Ice Pack

≥ 2 years