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P6499 Sigma-Aldrich

PNU-282987 hydrate

solid, ≥98% (HPLC)

Synonym: 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)

  •  PubChem Substance ID 24898770

  •  NACRES NA.77

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Properties

Related Categories Agonists, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
InChI Key   OCWLMMBVXIESNP-GXKRWWSZSA-N
assay   ≥98% (HPLC)
form   solid
storage condition   desiccated
solubility   DMSO: >10 mg/mL
storage temp.   2-8°C

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.

Packaging

10, 50 mg in glass bottle

Biochem/physiol Actions

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.

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.

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.

Caution

Air sensitive

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis (COA)

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Certificate of Origin (COO)

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Protocols & Articles

Articles

Acetylcholine Receptors (Nicotinic)

Nicotinic acetylcholine receptors (nAChRs) constitute a family of ligand-gated channels, originally classified on the basis of their activation by the alkaloid nicotine, with acetylcholine (ACh) bein...
Keywords: Analgesics, Diseases, Dopamine agents, Gene expression, Genetic, Inflammation, Ligands, Microscopy, Neurotransmission, Neurotransmitters, Scanning electron microscopy, Schizophrenia, Tissue microarrays, Transduction

Peer-Reviewed Papers
15

References

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