PNU-282987 hydrate
SIGMA/P6499 - solid, ≥98% (HPLC)
Synonym: N-
Empirical Formula (Hill Notation): C14H17ClN2O · HCl · xH2O
Molecular Weight: 301.21 (anhydrous basis)
Linear Formula: C14H17ClN2O · HCl · xH2O
Product Type: Chemical
| assay | ≥98% (HPLC) |
| form | solid |
| InChI | 1S/C14H17ClN2O.ClH.H2O/c1 |
| InChI key | OCWLMMBVXIESNP-GXKRWWSZSA |
| Quality Level | 200  |
| SMILES string | Cl[H].[H]O[H].Clc1ccc(cc1 |
| solubility | DMSO: >10 mg/mL |
| storage condition | desiccated |
| storage temp. | 2-8°C |
| 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: | 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. |
| 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. |
| Biochem/physiol Actions: | Selective α7 nicotinic receptor agonist. Ki = 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. |
| Disclaimer: | 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 . |
| Other Notes: | 2024 CiteAb Award Winner for Supplier Succeeding in Parkinson′s Research  |
| Packaging: | 10, 50 mg in glass bottle |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |