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4-PPBP maleate

Names

[ CAS No. ]:
201216-39-9

[ Name ]:
4-PPBP maleate

[Synonym ]:
4-Phenyl-1-(4-phenylbutyl)piperidine (2Z)-but-2-enedioate (1:1)
4-Phenyl-1-(4-phenylbutyl)piperidine (2Z)-2-butenedioate (1:1)
Piperidine, 4-phenyl-1-(4-phenylbutyl)-, (2Z)-2-butenedioate (1:1)

Biological Activity

[Description]:

4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection[1][2][3].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Sigma Receptor
Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[In Vitro]

4-PPBP maleate elicits ERK1/2 phosphorylation in primary neurons[3].

[In Vivo]

4-PPBP maleate (1 μmol/kg; i.v.) decreases brain injury after transient focal ischemia in rats[2]. Animal Model: Male rats weighing 300 to 385 g (Transient focal ischemia model)[2] Dosage: 1 μmol/kg Administration: Per hour by continuous intravenous infusion starting 1 hour after the initiation of ischemia and continuing through 22 hours of reperfusion. Result: Decreased brain injury after transient focal ischemia in rats.

[References]

[1]. Whittemore ER, et al. Antagonism of N-methyl-D-aspartate receptors by sigma site ligands: potency, subtype-selectivity and mechanisms of inhibition. J Pharmacol Exp Ther. 1997;282(1):326-338.

[2]. Takahashi H, et al. PPBP [4-phenyl-1-(4-phenylbutyl) piperidine] decreases brain injury after transient focal ischemia in rats. Stroke. 1996;27(11):2120-2123.

[3]. Tan F, et al. The σ 1 receptor agonist 4-PPBP elicits ERK1/2 phosphorylation in primary neurons: a possible mechanism of neuroprotective action. Neuropharmacology. 2010;59(6):416-424.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H31NO4

[ Molecular Weight ]:
409.518

[ Exact Mass ]:
409.225311


Related Compounds