Capsaicin, Nociception and Pain

Frias, B.; Merighi, Adalberto

doi:10.3390/molecules21060797

Cited by 183 publications

(151 citation statements)

References 254 publications

(304 reference statements)

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“…It should be considered that vocalizations can be a response to pain (Palmer, 2005) provoked by the application of the electric pulses during EEP in rams (Damián & Ungerfeld, 2011) and deer (Fumagalli et al, 2015). Presumably, rams are more sensitive to pain during electric stimulation: while prostate and the stimulated region in males has nociceptive receptors of pain (Frias & Merighi, 2016), the vagina has not. Another non-opposed explanation is that sexual and probably genital stimulation triggered the emission of vocalizations in rams (Patel, Das, Pandey, Yadav, & Girish, 2005), as it provoked the erection, protrusion of the penis and ejaculation.…”

Section: Discussionmentioning

confidence: 99%

Ejaculation does not contribute to the stress response to electroejaculation in sheep

Abril-Sánchez

Freitas‐de‐Melo

Damián

et al. 2017

Reprod Domestic Animals

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Electroejaculation procedures (EEPs) provoke stress; nevertheless, ejaculation produces physiological changes similar as those usually used to measure stress responses. The application of EEP to animals that cannot ejaculate-as ewes-may be useful to discriminate the responses induced by ejaculation from those provoked by EEP. The aim was to determine the stress response to EEP in rams and ewes. The EEPs were applied to 10 rams and 10 ewes during the non-breeding season, and the number of vocalizations, the heart rate, rectal temperature, serum cortisol concentration, biochemical and haematological parameters were measured. Overall, EEP provoked increases in cortisol concentration, glycaemia, rectal temperature and concentration of creatine kinase (all them: p < .0001) as well as relative concentration of granulocytes (p = .003) and absolute granulocyte concentration (p = .0002) in both, rams and ewes. Heart rate, relative concentration of lymphocytes (p = .001), haematocrit (p = .02) and haemoglobin (p = .045) decreased in animals from both genders after EEP. Besides, cortisol (p < .0001), rectal temperature (p = .002) and glycaemia (p = .001) were greater in ewes than rams, and creatine kinase also tended to be greater in ewes than rams (p = .054). On the other hand, the number of animals that vocalized (p = .006), white blood cells (p = .02) and absolute lymphocytes (p = .02) were greater in rams than ewes. The general trends show a similar pattern of stress responses in animals from both genders. Therefore, we concluded that ejaculation does not contribute to the stress response provoked by the EEP. This procedure also provokes muscular damage and probably pain.

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Section: Discussionmentioning

confidence: 99%

Ejaculation does not contribute to the stress response to electroejaculation in sheep

Abril-Sánchez

Freitas‐de‐Melo

Damián

et al. 2017

Reprod Domestic Animals

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“…This results in the reduction of TRPV1 activation when the cells are near to the resting potential . A series of TRPV1 exogenous agonists such as vanilloids (e.g., olvanil, resiniferatoxin, RTX), capsinoids (e.g., capsiate), camphor, heat (>43°C) and pH (<5.9), endogenous agonists (e.g., anandamide), lipoxygenase products(e.g., LTB4), N ‐acyldopamines, and endogenous modulators (such as PAR‐2 agonists, nerve growth factor [NGF], ATP) have been characterized . (Figure )…”

Section: Structure Regulation and Distributionmentioning

confidence: 99%

Medicinal Chemistry, Pharmacology, and Clinical Implications of TRPV1 Receptor Antagonists

Tabrizi

Baraldi

et al. 2016

Medicinal Research Reviews

129

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Transient receptor potential vanilloid 1 (TRPV1) is an ion channel expressed on sensory neurons triggering an influx of cations. TRPV1 receptors function as homotetramers responsive to heat, proinflammatory substances, lipoxygenase products, resiniferatoxin, endocannabinoids, protons, and peptide toxins. Its phosphorylation increases sensitivity to both chemical and thermal stimuli, while desensitization involves a calcium-dependent mechanism resulting in receptor dephosphorylation. TRPV1 functions as a sensor of noxious stimuli and may represent a target to avoid pain and injury. TRPV1 activation has been associated to chronic inflammatory pain and peripheral neuropathy. Its expression is also detected in nonneuronal areas such as bladder, lungs, and cochlea where TRPV1 activation is responsible for pathology development of cystitis, asthma, and hearing loss. This review offers a comprehensive overview about TRPV1 receptor in the pathophysiology of chronic pain, epilepsy, cough, bladder disorders, diabetes, obesity, and hearing loss, highlighting how drug development targeting this channel could have a clinical therapeutic potential. Furthermore, it summarizes the advances of medicinal chemistry research leading to the identification of highly selective TRPV1 antagonists and their analysis of structure-activity relationships (SARs) focusing on new strategies to target this channel.

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“…Both antagonism and agonism of the TRP channel are critical pharmacological approaches for pain management [45][46][47][48]. For example, TRPV1 antagonism has utility in acute analgesia but chronic pain management requires longer-term strategies such as receptor and neuronal desensitization using TRPV1 agonists.…”

Section: Introductionmentioning

confidence: 99%

Diverse TRPV1 responses to cannabinoids

et al. 2019

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Cannabinoid compounds are potential analgesics. Users of medicinal Cannabis report efficacy for pain control, clinical studies show that cannabis can be effective and opioid sparing in chronic pain, and some constituent cannabinoids have been shown to target nociceptive ion channels. Here, we explore and compare a suite of cannabinoids for their impact upon the physiology of TRPV1. The cannabinoids tested evoke differential responses in terms of kinetics of activation and inactivation. Cannabinoid activation of TRPV1 displays significant dependence on internal and external calcium levels. Cannabinoid activation of TRPV1 does not appear to induce the highly permeant, pore-dilated channel state seen with Capsaicin, even at high current amplitudes. Finally, we analyzed cannabinoid responses at nociceptive channels other than TRPV1 (TRPV2, TRPM8, and TRPA1), and report that cannabinoids differentially activate these channels. On the basis of response activation and kinetics, state-selectivity and receptor selectivity, it may be possible to rationally design approaches to pain using single or multiple cannabinoids.

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Capsaicin, Nociception and Pain

Cited by 183 publications

References 254 publications

Ejaculation does not contribute to the stress response to electroejaculation in sheep

Ejaculation does not contribute to the stress response to electroejaculation in sheep

Medicinal Chemistry, Pharmacology, and Clinical Implications of TRPV1 Receptor Antagonists

Diverse TRPV1 responses to cannabinoids

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