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Acta Biomedica Scientia

Volume 4, Issue 3, 2017
Mcmed International
Acta Biomedica Scientia
Issn
2348 - 215X (Print), 2348 - 2168 (Online)
Frequency
bi-annual
Email
editorabs@mcmed.us
Journal Home page
http://mcmed.us/journal/abs
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Abstract
Title
LIPOXYGENASE-DERIVED METABOLITES 9-HODE AND 13- HODE AS MODULATORS OF TRPV1 ACTIVITY: IMPLICATIONS FOR PAIN AND INFLAMMATION
Author
Dr. Amaranath Reddy K
Email
keyword
TRPV1 ion channel, 9-HODE, Anandamide, TRP channels, Pain signaling.
Abstract
This study investigates the pharmacological properties of lipoxygenase-derived metabolites, particularly 9-HODE and 13- HODE, in modulating the activity of the transient receptor potential vanilloid-1 (TRPV1) ion channel, a key player in pain signaling and neurogenic inflammation. Through fluorescence-based calcium imaging in cells overexpressing TRPV1, the study explores the potency, efficacy, and desensitization potential of 9-HODE enantiomers in comparison with anandamide, a well-known TRPV1 agonist. The findings reveal that 9(S)-HODE exhibits higher efficacy and potency in rat TRPV1 channels than 9(R)-HODE, though its activity in human TRPV1 is comparatively weaker. Additionally, 9-HODE demonstrated partial desensitization of TRPV1, with a concentration-dependent response observed in dorsal root ganglion (DRG) neurons. Unlike anandamide, which is selectively active at TRPV1, HODEs also interact with other TRP channels, including TRPA1, TRPV2, and TRPM8. These results highlight the potential of lipoxygenase metabolites in modulating pain pathways, offering new insights into their role in inflammatory pain and neurogenic inflammation. The study further suggests that experimental conditions, such as assay endpoints and temperature, can significantly influence the potency of TRPV1 agonists, underlining the complexity of their therapeutic potential.
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