Abstract
Nowadays, a significant number of antiepileptic drugs aimed at influencing the main inhibitory transmitter – gamma-aminobutyric acid (GABA). Compounds with various chemical structures, binding to different GABAA sites, potentiate the action of amino acid. Recent studies have reported that phenolic compounds such as vanillin and its derivatives also have actions within the CNS and act as enhancer of GABA potential. On the other hand, vanillin affects the peripheral nervous system as agonist of TRPV1 channels that are involved in the transmission and modulation of pain (nociception) as well as the integration of diverse painful stimuli. At the present study, the influence of vanillin and its derivatives (vanillin oxime, vanillyl alcohol and vanillic acid) on the central and peripheral nervous system was reliably confirmed by evaluating their anticonvulsant, antidepressant and analgesic activity. The present findings indicate that all aforementioned compounds possess antiseizure action after oral administration on PTZ-induced convulsion model. Antidepressant activity, studied by forced swimming test (FST), has been more pronounced manifested for vanillin and vanillic acid during 24 hours after administration. Intriguingly, TRPV1 agonist vanillin and its oxime after transdermal delivery produced hyperalgesia when tested on allylisothiocyanate- and capsaicin-induced models, whereas vanillyl alcohol and vanillic acid were found to reduce the pain sensation.
Highlights
The identification and structure determination of novel pharmacological targets ‒ transient receptor potential (TRP) ion channels ‒ provides an opportunity for the rational design and synthesis of TRP modulators
The present findings indicate that all aforementioned compounds possess antiseizure action after oral administration on pentylenetetrazole model (PTZ)-induced convulsion model
TRPV1 agonist vanillin and its oxime after transdermal delivery produced hyperalgesia when tested on allylisothiocyanate- and capsaicin-induced models, whereas vanillyl alcohol and vanillic acid were found to reduce the pain sensation
Summary
The identification and structure determination of novel pharmacological targets ‒ transient receptor potential (TRP) ion channels ‒ provides an opportunity for the rational design and synthesis of TRP modulators. Numerous studies have shown that representatives of various TRP channel subfamilies are involved in pain perception and inflammatory processes. In this context, TRPA1 and TRPV1 channels are of paramount interest to pharmacologists and practicing surgeons since antagonists of aforementioned receptors are considered promising drugs undergoing clinical trials. TRPA1 and TRPV1 channels are of paramount interest to pharmacologists and practicing surgeons since antagonists of aforementioned receptors are considered promising drugs undergoing clinical trials These receptors have been established as molecular targets for a variety of phytochemicals among which special attention is paid to phenolic compounds such as vanillin and its derivatives. Vanillin simultaneously affects both central and peripheral nervous system
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
