- Histamine H3 Inverse Agonists and Antagonists and Methods of Use Thereof
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Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
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Page/Page column 66
(2011/04/18)
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- Synthesis of epibatidine isomers: endo-5- and 6- (6′-chloro-3′-pyridyl-2-azabicyclo[2.2.1]heptanes
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Synthesis of the title compounds is described; detailed NMR data are provided in support of the proposed stereostructures. The 5- and 6-endo-compounds show high selectivity for α4β2 versus α7 nAChR subtypes; in contrast, the exo-stereoisomers show compara
- Cox,Malpass,Gordon,Rosen
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p. 2372 - 2379
(2007/10/03)
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- Synthesis and Muscarinic Receptor Activity of Ester Derivatives of 2-Substituted 2-Azabicycloheptan-5-ol and -6-ol
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Radioligand binding affinities of four new muscarinic antagonists and six potential muscarinic agonists which possess the 2-alkyl-2-azabicycloheptane ring system have been determined in rat heart, rat brain, and m1- or m3-tran
- Carroll, F. Ivy,Abraham, Phillip,Chemburkar, Sanjay,He, Xu-Chang,Mascarella, S. Wayne,et al.
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p. 2184 - 2191
(2007/10/02)
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