P6499

PNU-282987 hydrate

solid, ≥98% (HPLC)

• Synonym(s): N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chloro-benzamide monohydrochloride hydrate
• Empirical Formula (Hill Notation): C₁₄H₁₇ClN₂O · HCl · xH₂O
• Molecular Weight: 301.21 (anhydrous basis)
• UNSPSC Code: 12352200
• PubChem Substance ID: 24898770
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: desiccated

Properties

• Quality Segment: 200
• assay: ≥98% (HPLC)
• form: solid
• storage condition: desiccated
• solubility: DMSO: >10 mg/mL
• storage temp.: 2-8°C
• SMILES string: Cl[H].[H]O[H].Clc1ccc(cc1)C(=O)N[C@H]2CN3CCC2CC3
• InChI: 1S/C14H17ClN2O.ClH.H2O/c15-12-3-1-11(2-4-12)14(18)16-13-9-17-7-5-10(13)6-8-17;;/h1-4,10,13H,5-9H2,(H,16,18);1H;1H2/t13-;;/m0../s1
• InChI key: OCWLMMBVXIESNP-GXKRWWSZSA-N

Description

Application

PNU-282987 hydrate has been used to check its activity in wound repair by inhibiting AGE (advanced glycation end products)-mediated tumor necrosis factor-α (TNF-α) production in a streptozotocin (STZ)-induced diabetic mouse model. It has also been used to evaluate the effects of nicotinic α-7 acetylcholine receptor (nAChRα7) activation on non-diabetic wound healing.

Biochem/physiol Actions

PNU-282987 is an agonist of nicotinic α-7 acetylcholine receptor (nAChRα7). It helps to decrease acute lung injury (ALI), stimulated by lipopolysaccharide (LPS). PNU-282987 can increase GABAergic synaptic activity in brain slices and helps to bring back auditory gating deficits in anesthetized rats.

Decreased expression of a homomeric alpha7 nicotinic acetylcholine receptor (nAChR) is connected with inability to process sensory information in schizophrenia. PNU-282987 is a novel selective agonist of the alpha7 nAChR that evoked whole-cell currents from cultured rat hippocampal neurons that were sensitive to the selective alpha7 nAChR antagonist methyllycaconitine (MLA) and enhanced GABAergic synaptic activity. The alpha7 nAChR agonist PNU-282987 improves auditory gating and enhances hippocampal oscillatory activity. These results provide further support for the concept that drugs that selectively activate alpha7 nAChRs may offer a novel, potential pharmacotherapy in treatment of schizophrenia.

Selective α7 nicotinic receptor agonist. K_i = 27 nM; displays negligible blockade of α₁β₁γδ and α₃β₄ nAChRs (IC₅₀ = 60 mM); enhances GABAergic synaptic activity in the hippocampus in vitro and enhances amphetamine-induced hippocampal theta wave activity.

Features and Benefits

This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Other Notes

2024 CiteAb Award Winner for Supplier Succeeding in Parkinson′s Research

Disclaimer

Air sensitive

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable