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A-582941 dihydrochloride

CAS No. : 848591-90-2

MCE 站：A-582941 dihydrochloride

产品活性：A-582941 dihydrochloride 是一种有效的，选择性的和可透过血脑屏障的 α7 nAChR 的部分激动剂，在大鼠脑膜和人额叶皮层的 K_i 值分别为 10.8 nM 和 16.7 nM。A-582941 dihydrochloride 以 150 nM 的 K_i 值与人 5-HT₃ 受体结合。A-582941 dihydrochloride 具有研究与各种神经退行性疾病和精神疾病相关的认知缺陷的潜力。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling  |  GPCR/G Protein

作用靶点：nAChR  |  5-HT Receptor

In Vitro: A-582941 (0.1-100 μM) protects against cell death induced by NGF withdrawal in PC12 cells.
A‐582941 (100 nM) increases the number of inhibitory postsynaptic potentials (IPSCs) by 260±70%, the sum of amplitudes by 220±30%, and the sum of areas by 210±40%.
A‐582941 increases ERK1/2 phosphorylation with an EC₅₀ of 95 nM in PC12 cells.

In Vivo: A‐582941 (3 μM/kg, i.p. once daily for 3 d) induces a moderate increase in ACh release in the medial prefrontal cortex (mPFCx) of freely moving rats.
A‐582941 (0.01-1.00 μM/kg, i.p.) produces a dose‐dependent increase in ERK1/2 phosphorylation in the cingulate cortex and hippocampus, and increases cAMP response element‐binding protein (CREB) phosphorylation in the cingulate cortex in mice.
A‐582941 (0.1-1.0 μM/kg, i.p.) evokes dose‐dependent increases in Ser‐9 GSK‐3β phosphorylation in the mouse cingulate cortex.
A‐582941 shows high oral bioavailability (mouse ~100%, rat 90%, dog 22%, monkey 50%) and C_max (mouse 18, rat 114, dog 79, monkey 39 ng/mL) following oral administration (mouse 1.0, rat 6.2, dog 3.0, monkey 3.0 μM/kg).
A‐582941 shows terminal elimination half-lives (mouse 1.4, rat 1.5, dog 1.4, monkey 2.0 h), plasma clearance (mouse 7.9, rat 4.7, dog 5.3, monkey 1.6 L/h/kg) and volumes of distribution (mouse 11.4, rat 9.2, dog 7.9, monkey 3.9 L/kg) following intravenous administration (mouse 1.0, rat 6.2, dog 0.5, monkey 0.5 μM/kg).

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