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Your search keyword '"Feuerbach, Dominik"' showing total 8 results
Start Over Author "Feuerbach, Dominik" Publisher american chemical society
8 results on '"Feuerbach, Dominik"'

1. Interaction of selective serotonin reuptake inhibitors with neuronal nicotinic acetylcholine receptors

Author

Arias, Hugo R., Feuerbach, Dominik, Targowska-Duda, Katarzyna M., Russell, Megan, and Jozwiak, Krzysztof

Subjects
Fluoxetine -- Chemical properties, Ligand binding (Biochemistry) -- Analysis, Nicotinic receptors -- Chemical properties, Serotonin uptake inhibitors -- Chemical properties, Serotonin uptake inhibitors -- Structure, Serotonin -- Structure, Serotonin -- Chemical properties, Biological sciences, Chemistry
Abstract

[Ca.sup.2+] influx, radioligand binding, and molecular docking approaches are utilized to compare the interaction of fluoxetine and paroxetine, two selective serotonin reuptake inhibitors (SSRIs), with the human (h) [alpha]4[beta]2, [alpha]3[beta]4, and [alpha]7 nicotinic acetylcholine receptors (AChRs) in different conformational states. The results suggested that SSRIs inhibit the most important neuronal AChRs with potencies and affinities that are clinically relevant by binding to a luminal site that are shared with tricyclic antidepressants.

Published
2010

2. Different interaction between the agonist JN403 and the competitive antagonist methyllycaconitine with the human [alpha]7 nicotinic acetylcholine receptor

Author

Arias, Hugo R., Ruo-Xu Gu, Feuerbach, Dominik, and Dong-Qing Wei

Subjects
Dementia -- Physiological aspects, Dementia -- Genetic aspects, Methyl groups -- Structure, Methyl groups -- Chemical properties, Nicotinic receptors -- Chemical properties, Nicotinic receptors -- Structure, Biological sciences, Chemistry
Abstract

The interaction of the agonist JN403 with the human (h) [alpha]7 nicotinic acetylcholine receptor (AChR) was compared to that for the competitive antagonist methyllycaconitine (MLA) to study the receptor selectivity of JN403 on the h[alpha]7, h[alpha]3[beta]4, and h[alpha]4[beta]2 AChRs. The results provide insight into the significance of the higher receptor specificity of JN403 for the treatment of [alpha]7-related disorders, including dementias, pain-related ailments, depression, anxiety, and wound healing.

Published
2010

3. Interaction of bupropion with muscle-type nicotinic acetylcholine receptors in different conformational states

Author

Arias, Hugo R., Gumilar, Fernanda, Rosenberg, Avraham, Targowska-Duda, Katarzyna M., Feuerbach, Dominik, Jozwiak, Krzysztof, Moaddel, Ruin, Wainer, Irving W., and Bouzat, Cecilia

Subjects
Bupropion -- Chemical properties, Bupropion -- Structure, Ligand binding (Biochemistry) -- Analysis, Nicotinic receptors -- Structure, Nicotinic receptors -- Chemical properties, Serine -- Chemical properties, Biological sciences, Chemistry
Abstract

Structural and functional methods were used to characterize the binding sites and the mechanisms of inhibition of bupropion on muscle-type nicotinic acetylcholine receptors (AChRs). The results suggested that interaction of bupropion with a luminal binding domain shared with PCP, located between the serine and valine rings is mediated primarily by entropy-driven process.

Published
2009

8. Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.

Author

Schopfer U, Schoeffter P, Bischoff SF, Nozulak J, Feuerbach D, and Floersheim P

Subjects
Amino Acid Motifs, Binding Sites, Central Nervous System Diseases drug therapy, Crystallography, X-Ray, Estrogen Receptor beta, HeLa Cells, Humans, Ligands, Models, Chemical, Models, Molecular, Protein Structure, Tertiary, Receptors, Estrogen chemistry, Tumor Cells, Cultured, Central Nervous System Diseases metabolism, Receptors, Estrogen agonists, Thiophenes chemistry, Thiophenes pharmacology
Abstract

In an effort to identify selective ligands for the estrogen receptor subtype ERbeta, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assays in HeLa and SH-SY5Y cells, compounds were characterized as ERbeta-selective agonists. By targeting ERbeta in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of endometrial and breast cancer.

Published
2002
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