PNU-282987 hydrate, solid, >=98% (HPLC)

Stock Code: 3573541
Manufacturer Part No: P6499-50MG
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£823.18 (exc VAT) per 50MG
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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-? (TNF-?) production in a streptozotocin (STZ)-induced diabetic mouse model. It has also been used to evaluate the effects of nicotinic ?-7 acetylcholine receptor (nAChR?7) activation on non-diabetic wound healing.


Biochem/physiol Actions


PNU-282987 is an agonist of nicotinic ?-7 acetylcholine receptor (nAChR?7). 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.


Caution


Air sensitive


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.


Packaging


10, 50 mg in glass bottle

InChI keyOCWLMMBVXIESNP-GXKRWWSZSA-N
InChI1S/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
ManufacturerSIGMA-ALDRICH
Storage Temp.2-8°C
SolubilityDMSO: >10 mg/mL
Formsolid
Assay≥98% (HPLC)

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