Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation

2022 ◽  
pp. 114091
Author(s):  
Maria Dichiara ◽  
Antonia Artacho-Cordón ◽  
Rita Turnaturi ◽  
Miriam Santos-Caballero ◽  
Rafael González-Cano ◽  
...  
Keyword(s):  
Hydrogen Sulfide ◽  
Pain Treatment ◽  
Receptor Antagonists ◽  
Design Synthesis ◽  
Sigma 1 Receptor ◽  
Pharmacological Evaluation ◽  
Sigma 1 ◽  
Treatment Design

scholarly journals Sigma-1 receptor antagonists haloperidol and chlorpromazine modulate the effect of glutoxim on NA+ transport in frog skin

2019 ◽  
Vol 484 (5) ◽  
pp. 629-632
Author(s):  
Z. I. Krutetskaya ◽  
A. V. Melnitskaya ◽  
V. G. Antonov ◽  
A. D. Nozdrachev
Keyword(s):  
Voltage Clamp ◽  
Frog Skin ◽  
Na Transport ◽  
Receptor Antagonists ◽  
Sigma 1 Receptor ◽  
Voltage Clamp Technique ◽  
Frog Skin Epithelium ◽  
Sigma 1 ◽  
Immunomodulatory Drug ◽  
First Time

Using voltage-clamp technique, the involvement of sigma-1 receptors in immunomodulatory drug glutoxim regulation of Na+ transport in frog skin was investigated. We have shown for the first time that preincubation of the frog skin with sigma-1 receptor antagonists – haloperidol or chlorpromazine – attenuates the stimulatory effect of glutoxim on Na+ transport. The results suggest the possible involvement of the sigma-1 receptors in glutoxim effect on Na+transport in frog skin epithelium.

Preliminary in vitro assessment of pharmacokinetic drug-drug interactions of EST64401 and EST64514, two sigma-1 receptor antagonists

Xenobiotica ◽  
2020 ◽  
pp. 1-40
Author(s):  
Raquel F. Reinoso ◽  
Sandra Yeste ◽  
Eva Ayet ◽  
María José Pretel ◽  
Ariadna Balada ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Receptor Antagonists ◽  
Sigma 1 Receptor ◽  
Sigma 1 ◽  
In Vitro Assessment ◽  
Pharmacokinetic Drug

scholarly journals Sigma 1 Receptor Antagonists Inhibit Manic-Like Behaviors in Two Congenital Strains of Mice

2018 ◽  
Vol 21 (10) ◽  
pp. 938-948
Author(s):  
Pilar Sánchez-Blázquez ◽  
Elsa Cortés-Montero ◽  
María Rodríguez-Muñoz ◽  
Javier Garzón
Keyword(s):  
Receptor Antagonists ◽  
Sigma 1 Receptor ◽  
Sigma 1

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

2019 ◽  
Vol 144 ◽  
pp. 244-255 ◽  
Author(s):  
Darren M. Riddy ◽  
Anna E. Cook ◽  
David M. Shackleford ◽  
Tracie L. Pierce ◽  
Elisabeth Mocaer ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Histamine H3 Receptor ◽  
Sigma 1 Receptor ◽  
Receptor Affinity ◽  
Receptor Kinetics ◽  
H3 Receptor ◽  
Sigma 1 ◽  
Drug Receptor ◽  
Histamine H3

Design, Synthesis, and Pharmacological Evaluation of Piperidin-4-yl amino aryl sulfonamides: Novel, Potent, Selective, Orally Active, and Brain Penetrant 5-HT6 Receptor Antagonists

2012 ◽  
Vol 55 (21) ◽  
pp. 9255-9269 ◽  
Author(s):  
Ramakrishna Nirogi ◽  
Anil Shinde ◽  
Anand Daulatabad ◽  
Ramasastri Kambhampati ◽  
Parandhama Gudla ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
Orally Active

Development of Potential Therapeutics for Pain Treatment by Inducing the Sigma 1 receptor Antagonism – In silico Approach

2021 ◽  
Author(s):  
Velimir Perić ◽  
Mladjan Golubović ◽  
Milan Lazarević ◽  
Vesna Marjanović ◽  
Tomislav Kostić ◽  
...  
Keyword(s):  
In Silico ◽  
Pain Treatment ◽  
Treatment Approach ◽  
Research Paper ◽  
Qsar Modeling ◽  
Receptor Antagonism ◽  
Sigma 1 Receptor ◽  
Sigma 1 ◽  
Potential Therapeutics

The sigma 1 receptor antagonism is deemed a promising pain treatment approach. The research paper outlines conformational-independent QSAR modeling for a range of compounds which serve as sigma 1 receptor...

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