N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-4-CHLORO-BENZAMIDE MONOHYDROCHLORIDE HYDRATE

Uses

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.