Table 2.

α7-nAChR ligands that have been evaluated in human clinical trials for pro-cognitive effects

Compound Name	α7 nAChR activity & other actions	Clinical Stage	Clinical Endpoints	References
ABT-126	Partial agonist	Phase II	Cognition, Negative Symptomology	Haig et al., 2016; Haig et al., 2016; Haig et al., 2018
AQW051	Partial agonist	Phase II	Cognition, fMRI Brain Activation	Barch et al., 2016
AVL-3288	PAM	Phase Ib	Cognition, Auditory Sensory Gating Negative Symptomology	Gee et al., 2017; Kantrowitz et al., 2020
Cytidine 5’-diphosphocholine (CDP-choline)	Full agonist	Phase II	Cognition, Auditory Sensory Gating	Knott et al., 2015; Aidelbaum et al., 2018; Choueiry et al., 2019
DMXB-A (GTS-21)	Partial agonist	Phase II	Cognition, Auditory Sensory Gating, Negative Symptomology	Olincy et al., 2006; Freedman et al., 2008
Encenicline (EVP-6124)	Partial agonist/5-HT3 antagonist	Phase III	Cognition, Negative Symptomology	Keefe et al., 2015
Galantamine	PAM/acetylcholinesterase inhibitor	Phase II	Cognition, Auditory Sensory Gating, Negative Symptomology	Choueiry et al., 2019; Buchanan et al., 2017
JNJ-39393406	PAM	Phase Ib	Cognition,Auditory Sensory Gating, Smoking Cessation	Winterer et al., 2013; Perkins et al., 2018
RG3487	Partial agonist/5-HT3 antagonist	Phase II	Cognition, Negative Symptomology	Umbricht et al., 2014
Tropisetron	Partial agonist/5-HT3 antagonist	Phase II	Cognition, Auditory Sensory Gating, Negative Symptomology	Shiina et al., 2010; Zhang et al., 2012; Noroozian et al., 2013
TC-5619	Full agonist	Phase II	Cognition, Negative Symptomology	Lieberman et al., 2013