Abstract

Capsaicin, the pungent ingredient of the hot chili pepper, is known to act on the transient receptor potential cation channel vanilloid subfamily member 1 (TRPV1). TRPV1 is involved in somatic and visceral peripheral inflammation, in the modulation of nociceptive inputs to spinal cord and brain stem centers, as well as the integration of diverse painful stimuli. In this review, we first describe the chemical and pharmacological properties of capsaicin and its derivatives in relation to their analgesic properties. We then consider the biochemical and functional characteristics of TRPV1, focusing on its distribution and biological effects within the somatosensory and viscerosensory nociceptive systems. Finally, we discuss the use of capsaicin as an agonist of TRPV1 to model acute inflammation in slices and other ex vivo preparations.

Highlights

  • 2 receptor-mediated mechanisms are involved in the induction of phosphorylated extracellular signal-regulated kinase after stimulation of primary sensory neurons (PSNs) with capsaicin, an effect not solely directly linked to the binding of the vanilloid to TRPV1 channels [27]

  • Noxious stimuli are detected by nerve endings found throughout the body and originating from the PSNs, which represent the first element of a polyneuronal chain leading to the perception of pain

  • Vagal afferents originate from PSNs in nodose ganglion that project pain directly, several studies have documented that stimulation of the vagus nerve attenuates somatic and visceral pain [39]

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Summary

Chemical Features of Capsaicin

Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide—C18 H27 NO3 ) is a naturally occurring substance derived from the plants of the genus Capsicum, family Solanaceae. Capsaicin is a vanilloid as it contains a vanillyl group in its formula. Vanilloids belong to a class of organic chemicals referred to as protoalkaloids, i.e., alkaloids where nitrogen is located in the side chain. Alkaloids often contain other elements among which is oxygen, as is the case for capsaicin. The first isolation of the vanilloid from paprika and cayenne dates back to 1876 and was reported by Thresh [1]. The first study on capsaicin structure dates back to 1920 [2]. The commercial production of capsaicin from natural sources primarily involves its isolation from Capsicum spp.

Natural Sources of Capsaicin
Cloning and General Distribution of TRPV1
Functional Properties and Biological Effects of TRPV1
Other Molecular Targets of Capsaicin
Nociception and Pain
Somatic Pain Pathways
Visceral Pain Pathways
Capsaicin as an Analgesic Medication
Structure and Splice Variants of TRPV1
Biochemistry and Physiology of TRPV1
PSNs and Non-Neural Cells
Somatic Pathways
Visceral Pathways
Schematics
Experimental Modeling Nociception Using Capsaicin in Vitro and ex Vivo
Schematic
Findings
Therapeutic Use of Capsaicin
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