serotonin receptor binding
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2021 ◽  
Vol 7 (3) ◽  
pp. 190
Author(s):  
Yong-Sung Park ◽  
Subin Jang ◽  
Hyunkoo Lee ◽  
Suzie Kang ◽  
Hyewon Seo ◽  
...  

Pleurotus eryngii produces various functional molecules that mediate physiological functions in humans. Recently, we observed that P. eryngii produces molecules that have antidepressant functions. An ethanol extract of the fruiting body of P. eryngii was obtained, and the extract was purified by XAD-16 resin using an open column system. The ethanol eluate was separated by HPLC, and the fraction with an antidepressant function was identified. Using LC-MS, the molecular structure of the HPLC fraction with antidepressant function was identified as that of tryptamine, a functional molecule that is a tryptophan derivative. The antidepressant effect was identified from the ethanol extract, XAD-16 column eluate, and HPLC fraction by a serotonin receptor binding assay and a cell-based binding assay. Furthermore, a forced swimming test (FST) showed that the mice treated with purified fractions of P. eryngii exhibited decreased immobility time compared with nontreated mice. From these results, we suggest that the extract of P. eryngii has an antidepressant function and that it may be employed as an antidepressant health supplement.


RSC Advances ◽  
2021 ◽  
Vol 11 (17) ◽  
pp. 9837-9839
Author(s):  
Padmabati Mondal

Correction for ‘In silico decryption of serotonin–receptor binding: local non-covalent interactions and long-range conformational changes’ by Padmabati Mondal et al., RSC Adv., 2020, 10, 37995–38003, DOI: 10.1039/D0RA05559J.


RSC Advances ◽  
2020 ◽  
Vol 10 (62) ◽  
pp. 37995-38003
Author(s):  
Padmabati Mondal

This study is focused on identifying the main non-covalent interactions controlling the stability of serotonin–receptor complexes as well as the main conformational changes in the receptor due to serotonin–receptor binding.


2018 ◽  
Vol 25 (9) ◽  
pp. 1036-1045 ◽  
Author(s):  
Yasushi Ikarashi ◽  
Kyoji Sekiguchi ◽  
Kazushige Mizoguchi

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.


2011 ◽  
Vol 15 (04) ◽  
pp. 435-447 ◽  
Author(s):  
Mark D. Underwood ◽  
Suham A. Kassir ◽  
Mihran J. Bakalian ◽  
Hanga Galfalvy ◽  
J. John Mann ◽  
...  

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

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