The discovery of the benzazepine class of histamine H3 receptor antagonists

Wilson, David M.; Apps, James; Bailey, N.T.; Bamford, Mark J.; Beresford, I.J.M.; Briggs, Michael A.; Calver, Andrew R.; Crook, Barry; Davis, Robert P.; Davis, Susannah; Dean, David K.; Harris, Leanne; Heightman, Tom D.; Panchal, Terry; Parr, Christopher A.; Quashie, Nigel; Steadman, Jon G.A.; Schogger, Joanne; Sehmi, Sanjeet S.; Stean, Tania O.; Takle, Andrew K.; Trail, Brenda; White, Trevor; Witherington, Jason; Worby, Angela; Medhurst, Andrew D.

doi:10.1016/j.bmcl.2013.09.089

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Alzheimer's Disease1

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“…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).…”

Section: Alzheimer's Diseasementioning

confidence: 94%