25CN‐NBOH: A selective agonist for in vitro and in vivo investigations of the serotonin 2A receptor

ChemMedChem ◽  
2021 ◽  
Author(s):  
Emil Märcher-Rørsted ◽  
Anders A. Jensen ◽  
Jesper Langgaard Kristensen
Keyword(s):  
Serotonin 2A Receptor ◽  
Selective Agonist ◽  
Serotonin 2A

scholarly journals An improved, scalable synthesis of the selective serotonin 2A receptor agonist 25CN-NBOH

SynOpen ◽  
2021 ◽  
Author(s):  
Emil Marcher-Rørsted ◽  
Jitka Nykodemova ◽  
Jesper Langgaard Kristensen
Keyword(s):  
Receptor Agonist ◽  
Scientific Community ◽  
In Vitro Studies ◽  
Selective Serotonin ◽  
Serotonin 2A Receptor ◽  
Scalable Synthesis ◽  
Serotonin 2A

4-(2-((2-hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH) was first reported as a potent and highly selective serotonin 2A receptor (5-HT2AR) agonist in 2014. The compound has since found extensive use as a pharmacological tool in a variety of in vivo and in vitro studies. In the present study, we present an improved and scalable synthesis of 25CN-NBOH making this compound readily available to the scientific community.

Further pharmacological evaluation of a novel synthetic peptide bradykinin B2 receptor agonist

2013 ◽  
Vol 394 (3) ◽  
pp. 353-360 ◽  
Author(s):  
Martin Savard ◽  
Julie Labonté ◽  
Céléna Dubuc ◽  
Witold Neugebauer ◽  
Pedro D’Orléans-Juste ◽  
...  
Keyword(s):  
Knockout Mice ◽  
Synthetic Peptide ◽  
Receptor Agonist ◽  
Rabbit Lung ◽  
Hypotensive Action ◽  
Duration Of Action ◽  
Selective Agonist ◽  
Comparable Magnitude

Abstract We recently identified a novel human B2 receptor (B2R) agonist [Hyp3,Thi5,NChg7,Thi8]-bradykinin (NG291) with greater in vitro and in vivo potency and duration of action than natural bradykinin (BK). Here, we further examined its stability and selectivity toward B2R. The hypotensive, antithrombotic, and profibrinolytic functions of NG291 relative to BK and its analogue ([Hyp3,Thi5,(4-Me)Tyr8(ΨCH2NH)Arg9]-BK) (RMP-7) were also tested. Contraction assays using isolated mouse stomachs (containing kinin B1R, B2R, and kininase I- and II-like activities) showed that NG291 is a more potent contractant than BK and is inhibited by HOE-140 (B2R antagonist) but unaffected by R954 (B1R antagonist), whereas both decreased the potency of BK. In stomach tissues from B2R knockout mice, BK maintained its activity via B1R, whereas NG291 had no contractile effect, indicating that it was selective for B2R. Unlike BK, NG291 was not degraded by rabbit lung ACE. Comparing intravenously administered BK and NG291 revealed that NG291 exhibited more potent and prolonged hypotensive action and greater antithrombotic and profibrinolytic activities. These effects were of comparable magnitude to RMP-7 and were absent in B2R knockout mice. We concluded that NG291 is a novel biostable B2R-selective agonist that may prove suitable for investigating the (pre)clinical cardioprotective efficacy of B2R activation.

P.107 Common HTR2A variants and 5-HTTLPR are not associated with in-vivo serotonin 2A receptor binding in healthy humans

2020 ◽  
Vol 31 ◽  
pp. S6-S7
Author(s):  
M. Spies ◽  
A. Nasser ◽  
B. Ozenne ◽  
P.S. Jensen ◽  
G.M. Knudsen ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Serotonin 2A Receptor ◽  
Healthy Humans ◽  
Serotonin 2A

Positive correlation between body mass index and in vivo serotonin 2A receptor binding in healthy humans

NeuroImage ◽  
2006 ◽  
Vol 31 ◽  
pp. T164
Author(s):  
David Erritzoe ◽  
V.G. Frokjaer ◽  
H. Arfan ◽  
S. Haugbol ◽  
L. Pinborg ◽  
...  
Keyword(s):  
Body Mass Index ◽  
Body Mass ◽  
Receptor Binding ◽  
Serotonin 2A Receptor ◽  
Positive Correlation ◽  
Healthy Humans ◽  
Serotonin 2A

SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo

1993 ◽  
Vol 237 (2-3) ◽  
pp. 299-309 ◽  
Author(s):  
André Bachy ◽  
Michel Héaulme ◽  
Antonina Giudice ◽  
Jean-Claude Michaud ◽  
Isabelle A. Lefevre ◽  
...  
Keyword(s):  
Selective Agonist

scholarly journals Serotonin 2A Receptor (5-HT2AR) Activation by 25H-NBOMe Positional Isomers: In Vitro Functional Evaluation and Molecular Docking

2021 ◽  
Vol 4 (2) ◽  
pp. 479-487 ◽  
Author(s):  
Eline Pottie ◽  
Olga V. Kupriyanova ◽  
Asher L. Brandt ◽  
Robert B. Laprairie ◽  
Vadim A. Shevyrin ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Functional Evaluation ◽  
Positional Isomers ◽  
Serotonin 2A Receptor ◽  
Serotonin 2A
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