scholarly journals Changes in TRPV1-Mediated Physiological Function in Rats Systemically Treated With Capsaicin on the Neonate

2020 ◽  
Vol 21 (9) ◽  
pp. 3143 ◽  
Author(s):  
Keun-Yeong Jeong

Capsaicin is the active component of chili peppers and is a hydrophobic, colorless, odorless, and crystalline to waxy compound. The transient receptor potential vanilloid 1 (TRPV1) is the capsaicin receptor channels that are involved in a variety of functions like transduction and transmission of the physiological stimulus. Subcutaneous injection of capsaicin to a newborn rat leads to involuntary lifelong TRPV1 desensitization. Various physiological changes including sensory and homeostatic actions in the body associated with neonatal capsaicin treatment are induced by direct TRPV1 channel targeting. Interesting changes include unique phenomena such as the reduction in pain perception, abnormal body temperature, increase in infection, infectious or neuropathological itching, and irregular circadian core body temperature rhythm. These symptoms are associated with relatively higher fever or loss of sensory c-fiber related to TRPV1 desensitization. The aforementioned outcomes not only provide a warning about the risk of capsaicin exposure in newborns but also indicate the possible occurrence of relatively rare diseases that are difficult to diagnose. Therefore, Therefore, the present review aims to summarize the unique phenomena caused by systemic capsaicin administration in neonatal rats.

2012 ◽  
Vol 342 (2) ◽  
pp. 416-428 ◽  
Author(s):  
Regina M. Reilly ◽  
Heath A. McDonald ◽  
Pamela S. Puttfarcken ◽  
Shailen K. Joshi ◽  
LaGeisha Lewis ◽  
...  

2020 ◽  
Vol 21 (21) ◽  
pp. 7942 ◽  
Author(s):  
Linda Rankin ◽  
Christopher J. Fowler

Palmitoylethanolamide (PEA, N-hexadecanoylethanolamide) is an endogenous compound belonging to the family of N-acylethanolamines. PEA has anti-inflammatory and analgesic properties and is very well tolerated in humans. In the present article, the basal pharmacology of PEA is reviewed. In terms of its pharmacokinetic properties, most work has been undertaken upon designing formulations for its absorption and upon characterising the enzymes involved in its metabolism, but little is known about its bioavailability, tissue distribution, and excretion pathways. PEA exerts most of its biological effects in the body secondary to the activation of peroxisome proliferator-activated receptor-α (PPAR-α), but PPAR-α-independent pathways involving other receptors (Transient Receptor Potential Vanilloid 1 (TRPV1), GPR55) have also been identified. Given the potential clinical utility of PEA, not least for the treatment of pain where there is a clear need for new well-tolerated drugs, we conclude that the gaps in our knowledge, in particular those relating to the pharmacokinetic properties of the compound, need to be filled.


2007 ◽  
Vol 35 (1) ◽  
pp. 115-119 ◽  
Author(s):  
J.P.H. Schoeber ◽  
J.G.J. Hoenderop ◽  
R.J.M. Bindels

Ca2+ is an essential ion in all organisms and many physiological functions in the body rely on the exact maintenance of the Ca2+ balance. The epithelial Ca2+ channels TRPV5 [TRP (transient receptor potential) vanilloid 5] and TRPV6 are the most Ca2+-selective members of the TRP superfamily and are generally considered as the gatekeepers of Ca2+ entry across epithelia. TRPV5 is involved in Ca2+ reabsorption from pro-urine, while TRPV6 has an essential role in intestinal Ca2+ uptake. These channels are the prime targets of calciotropic hormonal regulation, including vitamin D and parathyroid hormone. In addition, extra- and intra-cellular signalling by associated proteins and Ca2+ itself play key roles in TRPV5 and TRPV6 regulation. In this paper, we describe the present understanding of the concerted action of calbindin-D28k, klotho and BSPRY (B-box and SPRY-domain-containing protein) at different levels throughout the epithelial cell to control Ca2+ influx at the luminal entry gate.


2022 ◽  
Vol 2022 ◽  
pp. 1-7
Author(s):  
Chuanying Li ◽  
Rong Cheng ◽  
Lin Li ◽  
Miaomiao Chen ◽  
Cheng Wu

Duodenal ulcer seriously affects the quality of life and life safety of children, but the pathogenesis of children with duodenal ulcer is still unclear. As an important second messenger in the body, Ca2+ participates in the physiological and pathological processes of various diseases. Therefore, transient receptor potential vanilloid type 4 (TRPV4) as one of the channels that mediate Ca2+ has attracted widespread attention in recent years. Here, we found that TRPV4 is highly expressed in children with duodenal ulcer and has good diagnostic value through specimens of children with duodenal ulcer, and animal experiments have proved that TRPV4 is also highly expressed in duodenal ulcer mice. In addition, TRPV4 can enhance intestinal permeability, thereby promoting further infiltration of inflammatory factors. In summary, these results indicate that TRPV4 is involved in the occurrence and development of duodenal ulcer. Therefore, this study provides the diagnostic and therapeutic value of TRPV4 in children with duodenal ulcer.


2016 ◽  
Vol 96 (3) ◽  
pp. 911-973 ◽  
Author(s):  
John P. M. White ◽  
Mario Cibelli ◽  
Laszlo Urban ◽  
Bernd Nilius ◽  
J. Graham McGeown ◽  
...  

Transient receptor potential vanilloid type 4 (TRPV4) is a calcium-permeable nonselective cation channel, originally described in 2000 by research teams led by Schultz ( Nat Cell Biol 2: 695 –702, 2000) and Liedtke ( Cell 103: 525–535, 2000). TRPV4 is now recognized as being a polymodal ionotropic receptor that is activated by a disparate array of stimuli, ranging from hypotonicity to heat and acidic pH. Importantly, this ion channel is constitutively expressed and capable of spontaneous activity in the absence of agonist stimulation, which suggests that it serves important physiological functions, as does its widespread dissemination throughout the body and its capacity to interact with other proteins. Not surprisingly, therefore, it has emerged more recently that TRPV4 fulfills a great number of important physiological roles and that various disease states are attributable to the absence, or abnormal functioning, of this ion channel. Here, we review the known characteristics of this ion channel's structure, localization and function, including its activators, and examine its functional importance in health and disease.


Ból ◽  
2021 ◽  
Vol 22 (1) ◽  
pp. 56-65
Author(s):  
Małgorzata Malec-Milewska ◽  
Jerzy Wordliczek ◽  
Renata Zajączkowska

Neuropathic pain is still a challenging problem. It is experienced by millions of people worldwide, with an approximate prevalence of 7‒10% in the general population. Despite the availability of a variety of treatment methods, a significant proportion of patients suffer from poorly controlled neuropathic pain. Capsaicin is a highly selective TRPV1 (Transient Receptor Potential Vanilloid Type 1) agonist. When applied topically, it leads to the defunctionalisation of hyperactive nociceptive receptors, temporary destruction of peripheral nerve endings, and a significant reduction or cessation of pain. Therefore 8% capsaicin patches are used to treat several peripheral, localized neuropathic pain syndromes. The study aimed to present a case series of patients suffering from peripheral, localized neuropathic pain in case the use of repeated applications of 8% capsaicin patches significantly reduced the intensity of pain. In 5 out of 6 patients we observed a gradual extension of the pain relief period until the pain disappeared, which led to the reduction or discontinuation of systemic pharmacotherapy. In summary, a therapy limited to a certain area of the body, without potential systemic adverse effects, which requires repetition at fairly long intervals, appears to be a good treatment option.


Animals ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 2417
Author(s):  
Elout Van Liefferinge ◽  
Noémie Van Noten ◽  
Jeroen Degroote ◽  
Gunther Vrolix ◽  
Mario Van Poucke ◽  
...  

Transient receptor potential (TRP) channels contribute to sensory transduction in the body, agonized by a variety of stimuli, such as phytochemicals, and they are predominantly distributed in afferent neurons. Evidence indicates their expression in non-neuronal cells, demonstrating their ability to modulate gastrointestinal function. Targeting TRP channels could potentially be used to regulate gastrointestinal secretion and motility, yet their expression in the pig is unknown. This study investigated TRPA1 and TRPV1 expression in different gut locations of piglets of varying age. Colocalization with enteroendocrine cells was established by immunohistochemistry. Both channels were expressed in the gut mucosa. TRPV1 mRNA abundance increased gradually in the stomach and small intestine with age, most notably in the distal small intestine. In contrast, TRPA1 exhibited sustained expression across ages and locations, with the exception of higher expression in the pylorus at weaning. Immunohistochemistry confirmed the endocrine nature of both channels, showing the highest frequency of colocalization in enteroendocrine cells for TRPA1. Specific co-localization on GLP-1 immunoreactive cells indicated their possible role in GLP-1 release and the concomitant intestinal feedback mechanism. Our results indicate that TRPA1 and TRPV1 could play a role in gut enteroendocrine activity. Moreover, age and location in the gut significantly affected gene expression.


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