1. Membrane Transporter/Ion Channel
    Neuronal Signaling
    GPCR/G Protein
  2. nAChR
    5-HT Receptor
  3. A-582941 dihydrochloride

A-582941 dihydrochloride 

Cat. No.: HY-59201A
Handling Instructions

A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.

For research use only. We do not sell to patients.

A-582941 dihydrochloride Chemical Structure

A-582941 dihydrochloride Chemical Structure

CAS No. : 848591-90-2

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Description

A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research[1][2].

IC50 & Target[1]

α7 nAChR

10.8 nM (Ki, for rat α7 receptors)

α7 nAChR

16.7 nM (Ki, for human α7 receptors)

5-HT3 Receptor

150 nM (Ki)

In Vitro

A-582941 (0.1-100 μM) protects against cell death induced by NGF withdrawal in PC12 cells[2].
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%[2].
A‐582941 increases ERK1/2 phosphorylation with an EC50 of 95 nM in PC12 cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[2].
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[2].
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[2].
A‐582941 shows high oral bioavailability (mouse ~100%, rat 90%, dog 22%, monkey 50%) and Cmax (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)[2].
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)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley CD rats (250-275 g)[2]
Dosage: 3 μM/kg
Administration: I.p. once daily for 3 days
Result: Increased the releases of Ach.
The effect remained stable after the second and third administration.
Molecular Weight

353.29

Formula

C₁₇H₂₂Cl₂N₄

CAS No.

848591-90-2

SMILES

CN1CC(CN(C2=NN=C(C3=CC=CC=C3)C=C2)C4)C4C1.[H]Cl.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

A-582941A582941A 582941nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptorpartialα75-HT3cognitivedeficitsneurodegenerativepsychiatricInhibitorinhibitorinhibit

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A-582941 dihydrochloride
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