|EVP-6124 NAChRs agonist|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||550999-75-2||SDF||Download SDF|
|Solubility||DMSO||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
EVP-6124 is a partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs) that was proved high-affinity in vitro and in vivo. 
EVP-6124 was proved to show selectivity for α7 but low-affinity of α4β2 nAChRs in some binding and functional experiments. EVP-6124 had good brain penetration and an adequate exposure time. [1,2]
Co-administration of EVP-6124 and the selective nAChRs antagonist could contribute to the release of DA, ACH, and Glu. This could be used to treat cognitive impairment and possibly other dimensions of psychopathology. Co-administration of donepezil at 0.1 mg/kg, p.o. and EVP-6124 at 0.03 mg/kg proved to be fully restored memory while each of these did not improve memory in this task.  Pretreatment with the selective α7 nAChR antagonist, methyllycaconitine (MLA, 1.0 mg/kg), significantly blocked cortical DA and Glu efflux induced by EVP-6124 (0.1 mg/kg). [2,3]
1. Jos Prickaerts, Nick P. van Goethem, et al. EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. Neuropharmacology, 2012,62 (2): 1099-1110.
2. Mei Huang, Anna R. Felix, et al. Chaya Bhuvaneswaran, Dana Hilt, Gerhard K?nig, Herbert Y. Meltzer, The alpha-7 receptor agonist EVP-6124 increases dopamine and glutamate efflux in rat medial prefrontal cortex and nucleus accumbens. Biochemical Pharmacology, 2011, 82 (8): 1040.
3. Mei Huang, Anna R. Felix, et al. The novel α7 nicotinic acetylcholine receptor agonist EVP-6124 enhances dopamine, acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens. Psychopharmacology, 2014, 231:4541-4551.