A-582941 dihydrochloride_product_DataBase

Bioactivity	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].
Invitro	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].
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]. Animal Model:
Name	A-582941 dihydrochloride
CAS	848591-90-2
Formula	C17H22Cl2N4
Molar Mass	353.29
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Anderson DJ, et, al. [3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic receptor agonist: radioligand binding characterization to rat and human brain. J Pharm [2]. Tietje KR, et, al. Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties. CNS Neurosci Ther. Spring 2008; 14(1): 65-82.

PeptideDB

A-582941 dihydrochloride

CAS: 848591-90-2 F: C17H22Cl2N4 W: 353.29