Voltage-Activated Sodium Current Is Inhibited by Capsaicin in Rat Atrial Myocytes

Milesi, Verónica; Rebolledo, Alejandro; Alvis, Alicia Gómez; Raingo, Jesica; Gende, A. O. Grassi de

doi:10.1006/bbrc.2001.4688

Cited by 7 publications

(3 citation statements)

References 15 publications

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“…So far unequivocal identification of this receptor is restricted to primary afferent neurons and to neurons of the central nervous system (Caterina et al 1997;Mezey et al 2000), but there is growing evidence for its additional expression in non-neuronal cells (Bíró et al 1998a, b). In particular, functional studies provided evidence for the existence of at least one vanilloid receptor subtype in the rat heart (Gomez Alvis et al 1998;Milesi et al 2001;Yamato et al 1996). Rats exposed to an overdose of capsaicin die due to cardiorespiratory distress, and susceptibility to capsaicin changes during early postnatal life (Hiura et al 1992;Jancsó and Király 1981).…”

Section: Introductionmentioning

confidence: 99%

Transient expression of vanilloid receptor subtype 1 in rat cardiomyocytes during development

Dvoráková

Kummer

2001

Histochem Cell Biol

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Vanilloid receptor subtype 1 (VR1) is a non-selective cation channel detected on sensory neurons that is sensitive to capsaicin, the main pungent ingredient of hot chili pepper. Capsaicin application to neonatal animals causes cardiorespiratory distress, and this susceptibility to capsaicin changes during early postnatal life. This prompted us to hypothesise that in addition to its known neuronal localisation, VR1 is also expressed by non-neuronal cells of the heart during development. This issue was addressed in the rat heart during pre- and postnatal development by means of RT-PCR, western blot and immunohistochemistry. VR1-mRNA was transiently expressed from E14 to P30 but absent from adult hearts. Translation into protein was verified by western blotting. Immunohistochemistry proved that VR1 protein was localised in cardiomyocytes during those developmental stages at which mRNA was detected. In conclusion, VR1 is not neuron-specific but is transiently expressed on cardiomyocytes during ontogeny thereby pointing to a developmental role of this cation channel.

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Section: Introductionmentioning

confidence: 99%

Transient expression of vanilloid receptor subtype 1 in rat cardiomyocytes during development

Dvoráková

Kummer

2001

Histochem Cell Biol

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“…Capsaicin, at significantly higher concentrations, suppressed I Na , I L-Ca , I K1 with IC 50 values of 42.7 µM, 34.9 µM, and 38.8 µM, respectively. In an earlier study, capsaicin, at lower concentrations (0.4–4 µM), was reported to significantly suppress I Na in rat atrial myocytes [ 26 ]. Similarly, capsaicin, at a significantly lower concentration of 0.33 µM, inhibited Vmax during phase 0 of action potential in guinea-pig papillary muscle [ 10 ].…”

Section: Discussionmentioning

confidence: 99%

Capsaicin Inhibits Multiple Voltage-Gated Ion Channels in Rabbit Ventricular Cardiomyocytes in TRPV1-Independent Manner

et al. 2022

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Capsaicin is a naturally occurring alkaloid derived from chili pepper which is responsible for its hot, pungent taste. It exerts multiple pharmacological actions, including pain-relieving, anti-cancer, anti-inflammatory, anti-obesity, and antioxidant effects. Previous studies have shown that capsaicin significantly affects the contractility and automaticity of the heart and alters cardiovascular functions. In this study, the effects of capsaicin were investigated on voltage-gated ion currents in rabbit ventricular myocytes. Capsaicin inhibited rapidly activated (IKr) and slowly activated (IKs) K+ currents and transient outward (Ito) K+ current with IC50 values of 3.4 µM,14.7 µM, and 9.6 µM, respectively. In addition, capsaicin, at higher concentrations, suppressed voltage-gated Na+ and Ca2+ currents and inward rectifier IK1 current with IC50 values of 42.7 µM, 34.9 µM, and 38.8 µM, respectively. Capsaicin inhibitions of INa, IL-Ca, IKr, IKs, Ito, and IK1 were not reversed in the presence of capsazepine (3 µM), a TRPV1 antagonist. The inhibitory effects of capsaicin on these currents developed gradually, reaching steady-state levels within 3 to 6 min, and the recoveries were usually incomplete during washout. In concentration-inhibition curves, apparent Hill coefficients higher than unity suggested multiple interaction sites of capsaicin on these channels. Collectively, these findings indicate that capsaicin affects cardiac electrophysiology by acting on a diverse range of ion channels and suggest that caution should be exercised when capsaicin is administered to carriers of cardiac channelopathies or to individuals with arrhythmia-prone conditions, such as ischemic heart diseases.

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“…Direct actions of capsaicin on Na + channels are not limited to neurons. Milesi et al, 74 showed that in the concentration range of 0.4-4 µM, capsaicin inhibits VGSCs and the upstroke of the action potential in rat atrial myocytes, suggesting that the negative inotropic effect and antiarrhythmic properties of capsaicin [74][75][76] are related to its inhibitory actions on VGSCs in the rodent heart. Resiniferatoxin (RTX) is one of the most potent vanilloid agonists of TRPV1.…”

Section: Effects Of Capsaicinoids On Voltage-gated Sodium Channelsmentioning

confidence: 99%

Transient receptor potential vanilloid 1 (TRPV1)‐independent actions of capsaicin on cellular excitability and ion transport

Öz

Lorke

Howarth

2023

Medicinal Research Reviews

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Capsaicin is a naturally occurring alkaloid derived from chili pepper that is responsible for its hot pungent taste. Capsaicin is known to exert multiple pharmacological actions, including analgesia, anticancer, anti‐inflammatory, antiobesity, and antioxidant effects. The transient receptor potential vanilloid subfamily member 1 (TRPV1) is the main receptor mediating the majority of the capsaicin effects. However, numerous studies suggest that the TRPV1 receptor is not the only target for capsaicin. An increasing number of studies indicates that capsaicin, at low to mid µM ranges, not only indirectly through TRPV1‐mediated Ca2+ increases, but also directly modulates the functions of voltage‐gated Na+, K+, and Ca2+ channels, as well as ligand‐gated ion channels and other ion transporters and enzymes involved in cellular excitability. These TRPV1‐independent effects are mediated by alterations of the biophysical properties of the lipid membrane and subsequent modulation of the functional properties of ion channels and by direct binding of capsaicin to the channels. The present study, for the first time, systematically categorizes this diverse range of non‐TRPV1 targets and discusses cellular and molecular mechanisms mediating TRPV1‐independent effects of capsaicin in excitable, as well as nonexcitable cells.

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Voltage-Activated Sodium Current Is Inhibited by Capsaicin in Rat Atrial Myocytes

Cited by 7 publications

References 15 publications

Transient expression of vanilloid receptor subtype 1 in rat cardiomyocytes during development

Transient expression of vanilloid receptor subtype 1 in rat cardiomyocytes during development

Capsaicin Inhibits Multiple Voltage-Gated Ion Channels in Rabbit Ventricular Cardiomyocytes in TRPV1-Independent Manner

Transient receptor potential vanilloid 1 (TRPV1)‐independent actions of capsaicin on cellular excitability and ion transport

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