Výsledky vyhledávání - "Dennis B. McKay"

Akademický článek

Identification of a negative allosteric site on human α4β2 and α3β4 neuronal nicotinic acetylcholine receptors.

Autor: Ryan E Pavlovicz, Brandon J Henderson, Andrew B Bonnell, R Thomas Boyd, Dennis B McKay, Chenglong Li

Publikováno v: PLoS ONE, Vol 6, Iss 9, p e24949 (2011)

Acetylcholine-based neurotransmission is regulated by cationic, ligand-gated ion channels called nicotinic acetylcholine receptors (nAChRs). These receptors have been linked to numerous neurological diseases and disorders such as Alzheimer's disease,

Externí odkaz: https://doaj.org/article/9b57c8a5659c42d08cb4510e494a495c

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Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: Pharmacophore modeling and structure–activity relationship studies

Autor: Dennis B. McKay, Sihui Long, Tatiana F. González-Cestari, Bitna Yi, Ryan E. Pavlovicz, Chenglong Li, Karl A. Werbovetz, Brandon J. Henderson

Publikováno v: Bioorganic & Medicinal Chemistry. 21:4730-4743

The present study describes our ongoing efforts toward the discovery of drugs that selectively target nAChR subtypes. We exploited knowledge on nAChR ligands and their binding site that were previously identified by our laboratory through virtual scr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7735c40f7ae68b84d289740cfb364b08
https://doi.org/10.1016/j.bmc.2013.03.082

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3D-QSAR and 3D-QSSR models of negative allosteric modulators facilitate the design of a novel selective antagonist of human α4β2 neuronal nicotinic acetylcholine receptors

Autor: Dennis B. McKay, Stephen C. Bergmeier, Iwona Maciagiewicz, Brandon J. Henderson, Crina M. Orac

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:1797-1813

Subtype selective molecules for α4β2 neuronal nicotinic acetylcholine receptors (nAChRs) have been sought as novel therapeutics for nicotine cessation. α4β2 nAChRs have been shown to be involved in mediating the addictive properties of nicotine w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed8ed6240b0016d1e176ff2b681b1d0d
https://doi.org/10.1016/j.bmcl.2011.11.051

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Negative Allosteric Modulators That Target Human α4β2 Neuronal Nicotinic Receptors

Autor: R. Thomas Boyd, Dennis B. McKay, Jerad D. Allen, Stephen C. Bergmeier, Andrew B. Bonnell, Crina M. Orac, Tatiana F. González-Cestari, Michael X. Zhu, Chenglong Li, Brandon J. Henderson, Ryan E. Pavlovicz

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 334:761-774

Allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs) is considered to be one of the most promising approaches for therapeutics. We have previously reported on the pharmacological activity of several compounds that act as negat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8a7376360e4b92a73649f15e5855ea6
https://doi.org/10.1124/jpet.110.168211

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Effect of Novel Negative Allosteric Modulators of Neuronal Nicotinic Receptors on Cells Expressing Native and Recombinant Nicotinic Receptors: Implications for Drug Discovery

Autor: Crina M. Orac, R. Thomas Boyd, Dennis B. McKay, Michael X. Zhu, Raed A. El-Hajj, Stephen C. Bergmeier, Damon D. Reed, Brandon J. Henderson, Chenglong Li, Ryan E. Pavlovicz, Tatiana F. González-Cestari, Susan B. McKay, Aravinda B. Pulipaka

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 328:504-515

Allosteric modulation of nAChRs is considered to be one of the most promising approaches for drug design targeting nicotinic acetylcholine receptors (nAChRs). We have reported previously on the pharmacological activity of several compounds that seem

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c1ed6812b7bf07e01de04c8c04b8be5
https://doi.org/10.1124/jpet.108.144576

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Pharmacological and immunological identification of native α7 nicotinic receptors: Evidence for homomeric and heteromeric α7 receptors

Autor: Dennis B. McKay, Raed A. El-Hajj, Susan B. McKay

Publikováno v: Life Sciences. 81:1317-1322

Controversy surrounds the expression of alpha7 nicotinic acetylcholine receptors (nAChRs) in adrenal chromaffin cells. In these studies, alpha7 nAChRs expressed in bovine adrenal chromaffin cells are investigated. Using radiolabeled ligand binding te

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8abca42ceaf1964529cbb73fff82e5a
https://doi.org/10.1016/j.lfs.2007.08.039

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Analogs of Methyllycaconitine as Novel Noncompetitive Inhibitors of Nicotinic Receptors: Pharmacological Characterization, Computational Modeling, and Pharmacophore Development

Autor: Stephen C. Bergmeier, Dennis B. McKay, Susan B. McKay, Crina M. Orac, Michael X. Zhu, Kristjan M. Arason, Peter W. Swaan, Tatiana F. González-Cestari, Darrell L. Bryant, Aravinda B. Pulipaka, Cheng Chang, Raed A. El-Hajj

Publikováno v: Molecular Pharmacology. 71:1288-1297

As a novel approach to drug discovery involving neuronal nicotinic acetylcholine receptors (nAChRs), our laboratory targeted nonagonist binding sites (i.e., noncompetitive binding sites, negative allosteric binding sites) located on nAChRs. Cultured

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea5b8b472205366d32e4e0ca92a975f5
https://doi.org/10.1124/mol.106.033233

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Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the α3β4* nicotinic acetylcholine receptors through modifications to the ester

Autor: Susan B. McKay, Stephen C. Bergmeier, Darrell L. Bryant, Dennis B. McKay, K. A. Ismail, Kristjan M. Arason

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:3739-3742

The development of novel agents for the differentiation of neuronal nicotinic acetylcholine receptors (nAChRs) is important for the treatment of a variety of pathological conditions. We have prepared and evaluated a number of simpler analogues of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8eb266db48f9cf757dec018f1b022399
https://doi.org/10.1016/j.bmcl.2004.05.001

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Surface and intracellular nicotinic receptors expressed in intact adrenal chromaffin cells: direct measurements using [3H]epibatidine

Autor: R. Benjamin Free, Dennis B. McKay

Publikováno v: Brain Research. 974:60-69

The presence and importance of assembled, intracellular neuronal nicotinic acetylcholine receptors (nAChRs) has not been established in native systems. In these studies [3H]epibatidine binding techniques were used to characterize surface and intracel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1df164d05b99b56dabe43cb21a9c152
https://doi.org/10.1016/s0006-8993(03)02551-4

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