PHA-543613 (dihydrochloride)

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors[1]. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research[2][3].

Product Specifications

CAS Number

[478148-58-2]

UNSPSC

12352005

Target

NAChR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pha-543613-dihydrochloride.html

Purity

99.0

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC2=C(OC=C2)C=N1)N[C@H]3CN4CCC3CC4.[H]Cl.[H]Cl

Molecular Formula

C15H19Cl2N3O2

Molecular Weight

344.24

References & Citations

[1]Donn G Wishka, et al. Discovery of N-[ (3R) -1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. J Med Chem. 2006 Jul 13;49 (14) :4425-36.|[2]Nóra Bruszt, et al. Potentiation of cognitive enhancer effects of Alzheimer's disease medication memantine by alpha7 nicotinic acetylcholine receptor agonist PHA-543613 in the Morris water maze task. Psychopharmacology (Berl) . 2021 Nov;238 (11) :3273-3281.|[3]Krafft PR, et al. α7 nicotinic acetylcholine receptor agonism confers neuroprotection through GSK-3β inhibition in a mouse model of intracerebral hemorrhage. Stroke. 2012 Mar;43 (3) :844-50.