Henningfield, Jack E. Smith, Tracy T. Kleykamp, Bethea A. Fant, Reginald V. Donny, Eric C.
Published in
Psychopharmacology
Background and rationaleSteven R. Goldberg was a pioneering behavioral pharmacologist whose intravenous drug self-administration studies advanced the understanding of conditioned stimuli and schedules of reinforcement as determinants of pattern and persistence of drug-seeking behavior, and in particular, the importance of nicotine in tobacco use. H...
Comptour, Aurélie Rouzaire, Marion Belville, Corinne Bouvier, Damien Gallot, Denis Blanchon, Loïc Sapin, Vincent
Published in
Cellular and Molecular Life Sciences
Animal models of vitamin A (retinol) deficiency have highlighted its crucial role in reproduction and placentation, whereas an excess of retinoids (structurally or functionally related entities) can cause toxic and teratogenic effects in the embryo and foetus, especially in the first trimester of human pregnancy. Knock-out experimental strategies-t...
Mahemuti, Laziyan Chen, Qixuan Coughlan, Melanie C Zhang, Min Florian, Maria Mailloux, Ryan J Cao, Xu-Liang Scoggan, Kylie A Willmore, William G Jin, Xiaolei
...
Published in
Journal of environmental sciences (China)
Bisphenol A (BPA) has been shown to exert biological effects through estrogen receptor (ER)-dependent and ER-independent mechanisms. Recent studies suggest that prenatal exposure to BPA may increase the risk of childhood asthma. To investigate the underlying mechanisms in the actions of BPA, human fetal lung fibroblasts (hFLFs) were exposed to vary...
Achek, Asma Yesudhas, Dhanusha Choi, Sangdun
Published in
Archives of Pharmacal Research
The health of living organisms is constantly challenged by bacterial and viral threats. The recognition of pathogenic microorganisms by diverse receptors triggers a variety of host defense mechanisms, leading to their eradication. Toll-like receptors (TLRs), which are type I transmembrane proteins, recognize specific signatures of the invading micr...
Khanfar, Mohammad A Al-Qtaishat, Saja Habash, Maha Taha, Mutasem O
Published in
Chemico-biological interactions
Adenosine A2A receptor antagonists are of great interest in the treatment for Parkinson's disease. In this study, we combined extensive pharmacophore modeling and quantitative structure-activity relationship (QSAR) analysis to explore the structural requirements for potent Adenosine A2A antagonists. Genetic function algorithm (GFA) joined with k ne...
Sadek, Bassem Stark, Holger
Published in
Neuropharmacology
Histamine, a biogenic amine, is considered as a principle mediator of multiple physiological effects through binding to its H1, H2, H3, and H4 receptors (H1-H4Rs). Currently, the HRs have gained attention as important targets for the treatment of several diseases and disorders ranging from allergy to Alzheimer's disease and immune deficiency. Accor...
Fabritius, Charles-Henry Pesonen, Ullamari Messinger, Josef Horvath, Raymond Salo, Harri Gałęzowski, Michał Galek, Mariusz Stefańska, Klaudia Szeremeta-Spisak, Joanna Olszak-Płachta, Marta
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Published in
Bioorganic & medicinal chemistry letters
A series of 1-Sulfonyl-6-Piperazinyl-7-Azaindoles, showing strong antagonistic activity to 5-HT6 receptor (5-HT6R) was synthesized and characterized. The series was optimized to reduce activity on D2 receptor. Based on the selectivity against this off-target and the analysis of the ADME-tox profile, compound 1c was selected for in vivo efficacy ass...
Libbey, Jane E Hanak, Tyler J Doty, Daniel J Wilcox, Karen S Fujinami, Robert S
Published in
Experimental neurology
Seizures occur due to an imbalance between excitation and inhibition, with the balance tipping towards excitation, and glutamate is the predominant excitatory neurotransmitter in the central nervous system of mammals. Since upregulation of expression and/or function of glutamate receptors can contribute to seizures we determined the effects of thre...
Libbey, Jane E Hanak, Tyler J Doty, Daniel J Wilcox, Karen S Fujinami, Robert S
Published in
Experimental neurology
Seizures occur due to an imbalance between excitation and inhibition, with the balance tipping towards excitation, and glutamate is the predominant excitatory neurotransmitter in the central nervous system of mammals. Since upregulation of expression and/or function of glutamate receptors can contribute to seizures we determined the effects of thre...
Roshchina, Victoria V.
Published in
Journal of Fluorescence
Fluorescence as a parameter for analysis of intracellular binding and localization of neurotransmitters also named biomediators (acetylcholine and biogenic amines such as catecholamines, serotonin, histamine) as well as their receptors in plant cells has been estimated basing on several world publications and own experiments of the author. The subj...
