Kinetics, brain uptake, and receptor binding characteristics of flurazepam and its metabolites

1988 ◽  
Vol 94 (3) ◽  
Author(s):  
LawrenceG. Miller ◽  
DavidJ. Greenblatt ◽  
DarrellR. Abernethy ◽  
H. Friedman ◽  
MyDo Luu ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Brain Uptake ◽  
Binding Characteristics

scholarly journals Glucocorticoid receptor-binding characteristics in severe asthma

2003 ◽  
Vol 21 (6) ◽  
pp. 985-988 ◽  
Author(s):  
C. Bonnans ◽  
P. Chanez ◽  
H. Meziane ◽  
P. Godard ◽  
J. Bousquet ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Severe Asthma ◽  
Receptor Binding ◽  
Binding Characteristics

scholarly journals Comprehensive Structural and Molecular Comparison of Spike Proteins of SARS-CoV-2, SARS-CoV and MERS-CoV, and Their Interactions with ACE2

Cells ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 2638 ◽  
Author(s):  
Ma’mon M. Hatmal ◽  
Walhan Alshaer ◽  
Mohammad A. I. Al-Hatamleh ◽  
Malik Hatmal ◽  
Othman Smadi ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Binding Motif ◽  
Intermediate Hosts ◽  
Protein Structure Analysis ◽  
S Protein ◽  
Binding Characteristics ◽  
Protein Receptor ◽  
Genes Encoding ◽  
Tertiary Protein Structure ◽  
Molecular Comparison

The severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has recently emerged in China and caused a disease called coronavirus disease 2019 (COVID-19). The virus quickly spread around the world, causing a sustained global outbreak. Although SARS-CoV-2, and other coronaviruses, SARS-CoV and Middle East respiratory syndrome CoV (MERS-CoV) are highly similar genetically and at the protein production level, there are significant differences between them. Research has shown that the structural spike (S) protein plays an important role in the evolution and transmission of SARS-CoV-2. So far, studies have shown that various genes encoding primarily for elements of S protein undergo frequent mutation. We have performed an in-depth review of the literature covering the structural and mutational aspects of S protein in the context of SARS-CoV-2, and compared them with those of SARS-CoV and MERS-CoV. Our analytical approach consisted in an initial genome and transcriptome analysis, followed by primary, secondary and tertiary protein structure analysis. Additionally, we investigated the potential effects of these differences on the S protein binding and interactions to angiotensin-converting enzyme 2 (ACE2), and we established, after extensive analysis of previous research articles, that SARS-CoV-2 and SARS-CoV use different ends/regions in S protein receptor-binding motif (RBM) and different types of interactions for their chief binding with ACE2. These differences may have significant implications on pathogenesis, entry and ability to infect intermediate hosts for these coronaviruses. This review comprehensively addresses in detail the variations in S protein, its receptor-binding characteristics and detailed structural interactions, the process of cleavage involved in priming, as well as other differences between coronaviruses.

Structural modification of receptor-binding technetium-99m complexes in order to improve brain uptake

1997 ◽  
Vol 24 (3) ◽  
pp. 316-319 ◽  
Author(s):  
Bernd Johannsen ◽  
Ralf Berger ◽  
Peter Brust ◽  
Hans-Juergen Pietzsch ◽  
Matthias Scheunemann ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Structural Modification ◽  
Brain Uptake ◽  
Technetium 99M

scholarly journals Serotonin Receptor Binding Characteristics of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook

2018 ◽  
Vol 25 (9) ◽  
pp. 1036-1045 ◽  
Author(s):  
Yasushi Ikarashi ◽  
Kyoji Sekiguchi ◽  
Kazushige Mizoguchi
Keyword(s):  
Receptor Binding ◽  
Methyl Ether ◽  
Serotonin Receptor ◽  
Psychological Symptoms ◽  
Indole Alkaloid ◽  
Pharmacological Action ◽  
Antagonistic Activity ◽  
Receptor Subtypes ◽  
Binding Characteristics ◽  
Serotonin Receptor Binding

Background: Geissoschizine methyl ether (GM) is one of the indole alkaloids in Uncaria hook, and an active ingredient of yokukansan (YKS) that improves behavioral and psychological symptoms of dementia (BPSD) in patients with several types of dementia. The pharmacological action of GM has been related to various serotonin (5-HT) receptor subtypes. Objective: The aim of this article is to review the binding characteristics of GM to the 5-HT receptor subtypes in the brains using our own data and previous findings. Method: Competitive receptor-binding and agonist/antagonist activity assays for several 5-HT receptor subtypes were performed. Moreover, the articles describing pharmacokinetics and brain distribution of GM were searched in PubMed. Results: GM bound the following 5-HT receptor subtypes: 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5- HT4, 5-HT5A, 5-HT6, and 5-HT7. Among these receptors, GM had partial agonistic activity for 5-HT1A receptors and antagonistic activity for 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors. Also, GM was metabolized by various CYP isoforms, mainly CYP3A4. Parent/unchanged GM was detected in both the blood and brain of rats after oral administration of YKS. In the brains, GM was presumed to bind to 5- HT1A, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors on neuron-like large cells mainly in the frontal cortex. Conclusion: These results suggest that GM is a pharmacologically important alkaloid that regulates various serotonergic activities or functions by binding to multiple 5-HT receptor subtypes. Thus, this review provides recent 5-HT receptor-related evidence that GM is partly responsible for pharmacological effects of YKS.

Structural modification of receptor-binding technetium-99m complexes in order to improve brain uptake

1997 ◽  
Vol 24 (3) ◽  
pp. 316-319
Author(s):  
Bernd Johannsen ◽  
Ralf Berger ◽  
Peter Brust ◽  
Hans-Juergen Pietzsch ◽  
Matthias Scheunemann ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Structural Modification ◽  
Brain Uptake ◽  
Technetium 99M
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