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Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels
The histamine H3 receptor: an attractive target for the treatment of cognitive disorders
- T. Esbenshade, K. Browman, R. Bitner, M. Strakhova, M. Cowart, J. Brioni
- Biology, PsychologyBritish journal of pharmacology
- 1 July 2008
The purpose of this review is to acquaint the reader with the current understanding of H3 receptor localization and function as a modulator of neurotransmitter release and its effects on cognitive processes, as well as to provide an update on selected H3 antagonists in various states of preclinical and clinical advancement.
Discovery of Histamine H3 Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease
- J. Brioni, T. Esbenshade, T. Garrison, S. Bitner, M. Cowart
- Psychology, BiologyJournal of Pharmacology and Experimental…
- 1 January 2011
H3 antagonists exhibited wake-promoting effects in humans and efficacy in narcoleptic patients, indicating target engagement, but some of them were not efficacious in patients suffering from attention-deficit hyperactivity disorder and schizophrenic patients.
Localization of histamine H4 receptors in the central nervous system of human and rat
Diversity of neuronal nicotinic acetylcholine receptors: lessons from behavior and implications for CNS therapeutics.
Nicotinic receptor agonists exhibit anxiolytic-like effects on the elevated plus-maze test.
Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.
- J. Brioni, R. Moreland, J. Sullivan
- Biology, PsychologyProceedings of the National Academy of Sciences…
- 27 April 2004
The ability of ABT-724 to facilitate penile erection together with the favorable side-effect profile indicates that ABT -724 could be useful for the treatment of erectile dysfunction.
Central Mechanisms Regulating Penile Erection in Conscious Rats: The Dopaminergic Systems Related to the Proerectile Effect of Apomorphine
- G. Hsieh, P. R. Hollingsworth, J. Brioni
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 January 2004
The results suggest that the proerectile action of apomorphine in rats is mediated at supraspinal levels and that this effect is not mimicked by a D2 receptor agonist but associated with activation of D4 receptors.
Fatty acid amide hydrolase inhibitors display broad selectivity and inhibit multiple carboxylesterases as off-targets