6-[(3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254) is a novel histamine H 3 receptor antagonist with high affinity for human (pK i ϭ 9.59 -9.90) and rat (pK i ϭ 8.51-9.17) H 3 receptors. GSK189254 is Ͼ10,000-fold selective for human H 3 receptors versus other targets tested, and it exhibited potent functional antagonism (pA 2 ϭ 9.06 versus agonist-induced changes in cAMP) and inverse agonism [pIC 50 Progressive decline in cognitive performance is a key characteristic of Alzheimer's disease (AD) and related dementias, and improving cognitive function in these diseases represents a complex challenge, given the involvement of numerous neurotransmitter systems and brain regions (CoreyBloom, 2002). Current therapies, such as cholinesterase inhibitors, provide only minimal benefit to a subset of patients and for a limited period, so a number of alternative Article, publication date, and citation information can be found at

Within the criminal justice system, there is a growing trend toward utilizing videotape technology to record and to present confession evidence. Previous research, however, indicates that the point of view from which a confession is videotaped can influence determinations of its voluntariness. The present study extended this earlier result by demonstrating that (a) confessor‐focus, but not equal‐focus (on the confessor and interrogator), videotapes produce judgments of greater voluntariness compared to the more traditional audiotape and transcript formats; (b) this pattern generalizes across confessions concerned with three different crimes (i. e., rape, drug trafficking, and burglary); (c) individuals high and low in need for cognition are equally susceptible to the videotaped‐confession bias; and (d) biased voluntariness judgments may, in turn, prejudice likelihood‐of‐guilt assessments. In light of both a recent Supreme Court ruling stating that the improper use of involuntary confessions may in certain instances be considered “harmless error,” and the fact that actual criminal interrogations are usually videotaped with the focus on the confessor, these findings have important legal implications.

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We report the synthesis and SAR of a series of novel azaindole CB(2) agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive in a chronic model. 18 is a Pgp substrate with low brain penetration. The template was redesigned, and the resulting 5-azaindole 36 was a potent CB(2) agonist with high CNS penetration. This compound was efficacious in the acute model and the chronic joint pain model.

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