An approach for serotonin depletion in pigs: Effects on serotonin receptor binding

Synapse ◽  
2010 ◽  
Vol 65 (2) ◽  
pp. 136-145 ◽  
Author(s):  
Anders Ettrup ◽  
Birgitte R. Kornum ◽  
Pia Weikop ◽  
Gitte M. Knudsen
Keyword(s):  
Receptor Binding ◽  
Serotonin Receptor ◽  
Serotonin Depletion ◽  
Serotonin Receptor Binding

Ketanserin Analogs: The Effect of Structural Modification on 5-HT2 Serotonin Receptor Binding

1995 ◽  
Vol 38 (7) ◽  
pp. 1196-1202 ◽  
Author(s):  
Abd M. Ismaiel ◽  
Kim Arruda ◽  
Milt Teitler ◽  
Richard A. Glennon
Keyword(s):  
Receptor Binding ◽  
Structural Modification ◽  
Serotonin Receptor ◽  
Serotonin Receptor Binding

Platelet 5-HT2 serotonin receptor binding sites in autistic children and their first-degree relatives

1991 ◽  
Vol 30 (2) ◽  
pp. 121-130 ◽  
Author(s):  
Bruce D. Perry ◽  
Edwin H. Cook ◽  
Bennett L. Leventhal ◽  
Mark S. Wainwright ◽  
Daniel X. Freedman
Keyword(s):  
Receptor Binding ◽  
Binding Sites ◽  
Serotonin Receptor ◽  
Autistic Children ◽  
First Degree Relatives ◽  
Serotonin Receptor Binding

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.

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