Promising new receptor modulator affecting cognitive dysfunction

The alpha-7 nicotinic receptor (nAChR) is an acetylcholine receptor with implied importance for long-term memory and with a proposed role in neurological disorders such as Alzheimer’s disease and schizophrenia. In the recent study Pharmacological characterization of the novel and selective α7 nicotinic acetylcholine receptor positive allosteric modulator BNC375,  published in Journal of Pharmacology and Experimental Therapeutics, researchers from the Department of Neuroscience Research at Merck & Co. show that the nAChR positive allosteric modulator BNC375 selectively potentiates α7 nAChR currents with only marginal effects on receptor desensitization kinetics. Experiments in vivo also reveal positive cognitive effects of systemic administration of BNC375.

In their work, the researchers use Dynaflow Resolve to investigate the effect of BNC375 on in GH4C1 cells expressing rat α7 nAChR. The degree of potentiation was tested for different levels of BNC375 as well as the effect of BNC375 on the acetylcholine response curve. The results show that BNC375 has the capacity to increase the maximal response and potency of acetylcholine in stimulating α7 nAChR.

We are very happy to see that Wang et al. Have chosen to use Dynaflow Resolve in their work and hope that their findings will take us one step closer towards treatments that can improve cognitive function in patients with Alzheimer’s Disease.