We performed a clinical trial to evaluate the effects of the @entity112 subtype-3 receptor inverse agonist @entity59503 on cognition in @entity195 @entity1 . Mild-to-moderate @entity195 @entity1 were randomized 1:1 to 4 weeks of double-blind daily treatment with oral @entity59503 5-mg or placebo. Pharmacokinetic and PET data suggested that @entity59503 5-mg daily would achieve approximately 85% brain receptor occupancy at Cmax in elderly @entity1 . Primary efficacy measures were the short Computerized-Neuropsychological-Test-Battery (CNTB) summary score and @entity11509 -Cog score. A secondary efficacy measure was a Cognition Summary Score summarizing results from 7 cognitive tests. Of 144 @entity1 randomized, 132 completed 4 weeks ( @entity59503 = 65, placebo = 67). Most @entity1 (88.2%) were on concomitant symptomatic @entity195 treatment. There were no significant differences between treatments on primary and secondary endpoints at week 4: short CNTB summary score = 0.89 (95% CI: -0.74,2.52); @entity11509 -Cog score s -0.25 (95% CI: -1.61,1.11); Cognition Summary Score = 1.38 (95% CI: -0.64,3.40). @entity59503 was generally well tolerated but was associated with an increased percentage of @entity1 with adverse events (41/73; 56.2) versus placebo (18/70; 25.7%). Adverse events in > 5% of @entity1 on @entity59503 were @entity294 (8.2% vs. 2.9%), @entity10 (8.2% vs. 1.4%), @entity2473 (5.5% vs. 0%), @entity22 (5.5% vs. 0%) and stomach discomfort (5.5% vs. 0%). @entity59503 5-mg once daily over 4 weeks was not effective in improving cognitive function in mild to moderate @entity195 @entity1 who were on concomitant symptomatic @entity195 treatment. (ClinicalTrials.gov trial registration, NCT00420420).

Pilot randomized controlled study of a XXXX receptor inverse agonist in the symptomatic treatment of @entity195 .

@entity1 :: ('9606', 'Species') :: ['patients'] @entity11509 :: ('8540', 'Gene') :: ['ADAS'] @entity294 :: ('MESH:D003967', 'Disease') :: ['diarrhea'] @entity59503 :: ('MESH:C574738', 'Chemical') :: ['MK- 0249', 'MK-0249'] @entity112 :: ('MESH:D006632', 'Chemical') :: ['histamine'] @entity2473 :: ('MESH:D013035', 'Disease') :: ['muscle spasms'] @entity195 :: ('MESH:D000544', 'Disease') :: ['AD'] @entity10 :: ('MESH:D006261', 'Disease') :: ['headache'] @entity22 :: ('MESH:D007319', 'Disease') :: ['insomnia']
@entity112 :: (MESH:D006632,Chemical) :: ['histamine']
