“…Another two H3R antagonists, namely GSK-189254 and GSK-239512, have been described as potent, selective, and highly brain penetrant antagonists with proven effectiveness in a number of animal experiments, including attentional and memory models (Figure 10, Table 1) [53,59,[91][92][93][94][95][96][97]. Interestingly, GSK-239512 has completed phase 1 clinical trial, and the results suggest a modest efficacy in mild-moderate AD patients (ClinicalTrials.gov trial registration number: NCT00675090).…”