scholarly journals Synthesis and Evaluation of Novel α-Aminoamides Containing Benzoheterocyclic Moiety for the Treatment of Pain

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1716
Author(s):  
Kun Tong ◽  
Ruotian Zhang ◽  
Fengzhi Ren ◽  
Tao Zhang ◽  
Junlin He ◽  
...  
Keyword(s):  
Ion Channels ◽  
Patch Clamp ◽  
Formalin Test ◽  
Sodium Ion ◽  
Inhibitory Potency ◽  
Voltage Gated ◽  
Patch Clamp Electrophysiology ◽  
Sodium Ion Channels

Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds 6a, 6e, and 6f containing the benzofuran group displayed more potent in vivo analgesic activity than ralfinamide in both the formalin test and the writhing assay. Interestingly, they also exhibited potent in vitro anti-Nav1.7 and anti-Nav1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds 6a, 6e, and 6f, which have inhibitory potency for two pain-related Nav targets, could serve as new leads for the development of analgesic medicines.

scholarly journals Guanidinium Toxins and Their Interactions with Voltage-Gated Sodium Ion Channels

Marine Drugs ◽  
2017 ◽  
Vol 15 (10) ◽  
pp. 303 ◽  
Author(s):  
Lorena Durán-Riveroll ◽  
Allan Cembella
Keyword(s):  
Ion Channels ◽  
Sodium Ion ◽  
Voltage Gated ◽  
Sodium Ion Channels

Veratridine: A Janus-Faced Modulator of Voltage-Gated Sodium Ion Channels

2020 ◽  
Vol 11 (3) ◽  
pp. 418-426
Author(s):  
Robert A. Craig ◽  
Catherine E. Garrison ◽  
Phuong T. Nguyen ◽  
Vladimir Yarov-Yarovoy ◽  
J. Du Bois
Keyword(s):  
Ion Channels ◽  
Sodium Ion ◽  
Voltage Gated ◽  
Sodium Ion Channels

Diversity of Expression of the Sensory Neuron-Specific TTX-Resistant Voltage-Gated Sodium Ion Channels SNS and SNS2

2000 ◽  
Vol 15 (4) ◽  
pp. 331-342 ◽  
Author(s):  
Fumimasa Amaya ◽  
Isabelle Decosterd ◽  
Tarek A. Samad ◽  
Christopher Plumpton ◽  
Simon Tate ◽  
...  
Keyword(s):  
Ion Channels ◽  
Sensory Neuron ◽  
Sodium Ion ◽  
Voltage Gated ◽  
Sodium Ion Channels

scholarly journals Modeling and Bioinformatics Investigations of Human Voltage-gated Sodium Ion Channels

2014 ◽  
Vol 2 (2) ◽  
pp. 21-30
Author(s):  
Ali Jahanbazi Jahan Abad ◽  
Rahman Yolmeh ◽  
Fereshteh Parto ◽  
Abdorrahim Absalan ◽  
◽  
...  
Keyword(s):  
Ion Channels ◽  
Sodium Ion ◽  
Voltage Gated ◽  
Sodium Ion Channels

scholarly journals Fluorescent Saxitoxins for Live Cell Imaging of Single Voltage-Gated Sodium Ion Channels beyond the Optical Diffraction Limit

2012 ◽  
Vol 19 (7) ◽  
pp. 902-912 ◽  
Author(s):  
Alison E. Ondrus ◽  
Hsiao-lu D. Lee ◽  
Shigeki Iwanaga ◽  
William H. Parsons ◽  
Brian M. Andresen ◽  
...  
Keyword(s):  
Ion Channels ◽  
Live Cell Imaging ◽  
Cell Imaging ◽  
Diffraction Limit ◽  
Live Cell ◽  
Optical Diffraction ◽  
Sodium Ion ◽  
Voltage Gated ◽  
Sodium Ion Channels

scholarly journals Emerging Roles for Ion Channels in Ovarian Cancer: Pathomechanisms and Pharmacological Treatment

Cancers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 668
Author(s):  
Concetta Altamura ◽  
Maria Raffaella Greco ◽  
Maria Rosaria Carratù ◽  
Rosa Angela Cardone ◽  
Jean-François Desaphy
Keyword(s):  
Ovarian Cancer ◽  
Ion Channels ◽  
Transient Receptor Potential ◽  
Critical Role ◽  
Gynecologic Cancer ◽  
Receptor Potential ◽  
Transient Receptor Potential Channels ◽  
Platinum Resistance

Ovarian cancer (OC) is the deadliest gynecologic cancer, due to late diagnosis, development of platinum resistance, and inadequate alternative therapy. It has been demonstrated that membrane ion channels play important roles in cancer processes, including cell proliferation, apoptosis, motility, and invasion. Here, we review the contribution of ion channels in the development and progression of OC, evaluating their potential in clinical management. Increased expression of voltage-gated and epithelial sodium channels has been detected in OC cells and tissues and shown to be involved in cancer proliferation and invasion. Potassium and calcium channels have been found to play a critical role in the control of cell cycle and in the resistance to apoptosis, promoting tumor growth and recurrence. Overexpression of chloride and transient receptor potential channels was found both in vitro and in vivo, supporting their contribution to OC. Furthermore, ion channels have been shown to influence the sensitivity of OC cells to neoplastic drugs, suggesting a critical role in chemotherapy resistance. The study of ion channels expression and function in OC can improve our understanding of pathophysiology and pave the way for identifying ion channels as potential targets for tumor diagnosis and treatment.

Sign in / Sign up

Export Citation Format

Share Document