For research use only. Not for therapeutic Use.
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors[1]. PHA-543613 can be used for the cognitive deficits of Alzheimer’s disease and schizophrenia research[2].
PHA-543613 (0.3 mg/kg) successfully reverses Scopolamine-induced short-term memory deficits in rats[2].
PHA-543613 (4 and 12 mg/kg; i.p. once) reduces behavioral deficits and brain edema is dependent on the PI3K-Akt signaling pathway[3].
| Catalog Number | I008724 |
| CAS Number | 478149-53-0 |
| Synonyms | N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]furo[2,3-c]pyridine-5-carboxamide |
| Molecular Formula | C15H17N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C15H17N3O2/c19-15(12-7-11-3-6-20-14(11)8-16-12)17-13-9-18-4-1-10(13)2-5-18/h3,6-8,10,13H,1-2,4-5,9H2,(H,17,19)/t13-/m0/s1 |
| InChIKey | IPKZCLGGYKRDES-ZDUSSCGKSA-N |
| SMILES | C1CN2CCC1C(C2)NC(=O)C3=NC=C4C(=C3)C=CO4 |
| Reference | [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. |
