478148-58-2

478148-58-2 structure

Name: PHA-543613 Dihydrochloride
Chemical Name: PHA-543613 Dihydrochloride
CAS Number: 478148-58-2
Molecular Formula: C₁₅H₁₉Cl₂N₃O₂
Molecular Weight: 344.23600
Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
Create Date: 2017-11-29 02:31:00
Modify Date: 2024-01-03 19:46:51
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].

Name	PHA-543613 Dihydrochloride
Synonyms	N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]furo[2,3-c]pyridine-5-carboxamide

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR Signaling Pathways >> Neuronal Signaling >> nAChR Research Areas >> Neurological Disease
Target	Ki: 8.8 nM (α7 nAChR)[1]
In Vivo	PHA-543613 dihydrochloride (0.3 mg/kg) successfully reverses Scopolamine-induced short-term memory deficits in rats[2]. PHA-543613 dihydrochloride (4 and 12 mg/kg; i.p. once) reduces behavioral deficits and brain edema is dependent on the PI3K-Akt signaling pathway[3]. Animal Model: Male CD-1 mice with (intracerebral hemorrhage) ICH-induction or sham surgery[3] Dosage: 4 and 12 mg/kg Administration: Intraperitoneal injection; 4 and 12 mg/kg; 1 hour after surgery Result: Increased p-Akt and decreased p-GSK-3 and CC3 expressions in the ipsilateral hemisphere and reduced the neuronal cell death in the perihematomal area. Attenuated behavioral deficits andbrain edema at 72 hours after ICH.