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trpv1 blocker capsazepine (Tocris)

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Tocris trpv1 blocker capsazepine

Fig. 7 AEA analgesia and its interaction with <t>TRPV1</t> receptors. A Time courses of spike frequency (10-s bin size) induced by APs recorded from the peripheral part of trigeminal nerve innervating rat meninges within the 1-min active phase of the 2nd KCl pulse in combination with 10 µM AEA or with the co-application of 10 µM AEA and 20 µM capsazepine. Note the non-significant changes in nociceptive firing during applications of 10 µM AEA and the combination of 10 µM AEA and 20 µM capsazepine. Notably, capsaicin-induced firing decreased during the combined application of 10 µM AEA and 20 µM capsazepine. B No difference was observed between the APs ratio before and during 10 min capsazepine comparing to the Aps ratio of the same tine windows in the control condition. C The ratio of APs (before/during application of exogenous AEA, N = 5) for the 5-min baseline returned to the control baseline level in presence of capsazepine (N = 6, Mann Whitney U test, ** = 0.004). D The percentage between the number of APs induced by the 1st and 2nd KCl pulse for the 1-min within AEA was not affected by the application of both 10 µM AEA and 20 µM capsazepine. E The number of APs during the 1-min active phase of 1 µM Capsaicin when also AEA was applied (N=5) was reduced after application of both 10 µM AEA and 20 µM capsazepine (N = 6, Mann Whitney U test, ** = 0.008)

Trpv1 Blocker Capsazepine, supplied by Tocris, used in various techniques. Bioz Stars score: 95/100, based on 247 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/0464/Capsazepine/pm37038131-112-41-46
Average 95 stars, based on 247 article reviews

trpv1 blocker capsazepine - by Bioz Stars, 2026-09

95/100 stars

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1) Product Images from "Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain."

Article Title: Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain.

Journal: The journal of headache and pain

doi: 10.1186/s10194-023-01568-3

Fig. 7 AEA analgesia and its interaction with TRPV1 receptors. A Time courses of spike frequency (10-s bin size) induced by APs recorded from the peripheral part of trigeminal nerve innervating rat meninges within the 1-min active phase of the 2nd KCl pulse in combination with 10 µM AEA or with the co-application of 10 µM AEA and 20 µM capsazepine. Note the non-significant changes in nociceptive firing during applications of 10 µM AEA and the combination of 10 µM AEA and 20 µM capsazepine. Notably, capsaicin-induced firing decreased during the combined application of 10 µM AEA and 20 µM capsazepine. B No difference was observed between the APs ratio before and during 10 min capsazepine comparing to the Aps ratio of the same tine windows in the control condition. C The ratio of APs (before/during application of exogenous AEA, N = 5) for the 5-min baseline returned to the control baseline level in presence of capsazepine (N = 6, Mann Whitney U test, ** = 0.004). D The percentage between the number of APs induced by the 1st and 2nd KCl pulse for the 1-min within AEA was not affected by the application of both 10 µM AEA and 20 µM capsazepine. E The number of APs during the 1-min active phase of 1 µM Capsaicin when also AEA was applied (N=5) was reduced after application of both 10 µM AEA and 20 µM capsazepine (N = 6, Mann Whitney U test, ** = 0.008)

Figure Legend Snippet: Fig. 7 AEA analgesia and its interaction with TRPV1 receptors. A Time courses of spike frequency (10-s bin size) induced by APs recorded from the peripheral part of trigeminal nerve innervating rat meninges within the 1-min active phase of the 2nd KCl pulse in combination with 10 µM AEA or with the co-application of 10 µM AEA and 20 µM capsazepine. Note the non-significant changes in nociceptive firing during applications of 10 µM AEA and the combination of 10 µM AEA and 20 µM capsazepine. Notably, capsaicin-induced firing decreased during the combined application of 10 µM AEA and 20 µM capsazepine. B No difference was observed between the APs ratio before and during 10 min capsazepine comparing to the Aps ratio of the same tine windows in the control condition. C The ratio of APs (before/during application of exogenous AEA, N = 5) for the 5-min baseline returned to the control baseline level in presence of capsazepine (N = 6, Mann Whitney U test, ** = 0.004). D The percentage between the number of APs induced by the 1st and 2nd KCl pulse for the 1-min within AEA was not affected by the application of both 10 µM AEA and 20 µM capsazepine. E The number of APs during the 1-min active phase of 1 µM Capsaicin when also AEA was applied (N=5) was reduced after application of both 10 µM AEA and 20 µM capsazepine (N = 6, Mann Whitney U test, ** = 0.008)

Techniques Used: Control, MANN-WHITNEY

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Article Title: Hyperalgesic Effect Evoked by Il-16 and Its Participation in Inflammatory Hypernociception in Mice
Article Snippet: Mouse recombinant IL-16 (Raybiotech), the non-selective COX inhibitor diclofenac (Sigma), the selective COX-1 inhibitor SC-560 (Tocris) and the selective COX-2 inhibitor celecoxib (Sigma) were dissolved in saline. .. The TRPV1 antagonist capsazepine (Tocris) and the TRPA1 antagonist HC030031 (Tocris) were initially dissolved in DMSO and further diluted in saline up to a maximal DMSO concentration of 10%. .. The antibody against IL-16 (R&D, MAB1727) was initially reconstituted in PBS and next dissolved in saline.

Article Title: Unraveling the anti-primary dysmenorrhea mechanism of Ainsliaea fragrans Champ. extract by the integrative approach of network pharmacology and experimental verification.
Article Snippet: Background: The plant Ainsliaea fragrans Champ. (A. fragrans) named "Xingxiang Tuerfeng", is a traditional herb with a long history of therapeutic practice in southern China in the treatment of gynecological diseases.. Purpose: The anti-inflammatory extract of Ainsliaea fragrans Champ. (AF-ext) exhibited anti-primary dysmenorrhea (PD) activity in oxytocin-induced mice.. This study aimed to unravel the underlying mechanisms of AF-ext on PD by the integrative approach of network pharmacology and experimental verification.

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MS-induced ATP release is mediated by TRPM3 in GBM (A) Representative ATP traces recorded from naïve cells and cells pretreated with 200 μM 2-APB, 20 μM SKF-96365, 40 μM HC-030031, 100 μM quinine, 1 μM CBX, or 10 μM capsazepine for 10 min before MS. (B) Bar graph showing ATP responses ( ΔF/F₀ ) under each condition (2-APB, n = 10; SKF-96365, n = 6; HC-030031, n = 16; Quinine, n = 4; CBX, n = 4; capsazepine, n = 8). (C) Schematic of the vector constructs. (D) Relative mRNA expression levels of TRPM3, TRPM7, and TRPM8 in U-87 MG cells after shRNA-mediated knockdown, normalized to shSC. (E) Fluorescence images showing mCherry, GFP, and merged signals in U-87 MG cells infected with shTRPM3-mCherry. White arrows indicate representative cells. Scale bar = 50 μm. (F) Representative ATP traces recorded from U-87 MG (upper left), U-373 MG (lower left), and patient-derived GBM (lower right) cells infected with scrambled shRNA (shSC) or shTRPM3 #1. Representative ATP traces recorded from U-87 MG (upper, right) cells infected with shSC or shTRPM3 #2. (G) Bar graph comparing ATP responses ( ΔF/F₀ ) in each cell line (U-87 MG infected shTRPM3 #1, n = 28; U-87 MG infected shTRPM3 #2, n = 14; U-373 MG infected shTRPM3 #1, n = 10; patient-derived GBM infected shTRPM3 #1, n = 14). (H) Representative ATP traces recorded from U-87 MG cells infected with shSC or shTRPM7 (left) and corresponding bar graph comparing ATP responses ( ΔF/F₀ ) between shSC – and shTRPM7-infected cells (right) (n = 20 per condition). (I) Representative ATP traces recorded from U-87 MG cells infected with shSC or shTRPM8 (left) and corresponding bar graph comparing ATP responses ( ΔF/F₀ ) between shSC – and shTRPM8-infected cells (right) (n = 10 per condition). Each dot represents ATP responses of an individual cell. Data are presented as mean ± SEM. (B, D) Ordinary one-way ANOVA (Multiple comparisons). (G) Multiple Mann-Whitney tests. (H, I) Two-tailed unpaired t-test. * p < 0.05, ** p < 0.01, **** p < 0.0001.

Journal: Animal Cells and Systems

Article Title: ATP release mediated by TRPM3 enhances invasion in glioblastoma

doi: 10.1080/19768354.2026.2629066

Figure Lengend Snippet: MS-induced ATP release is mediated by TRPM3 in GBM (A) Representative ATP traces recorded from naïve cells and cells pretreated with 200 μM 2-APB, 20 μM SKF-96365, 40 μM HC-030031, 100 μM quinine, 1 μM CBX, or 10 μM capsazepine for 10 min before MS. (B) Bar graph showing ATP responses ( ΔF/F₀ ) under each condition (2-APB, n = 10; SKF-96365, n = 6; HC-030031, n = 16; Quinine, n = 4; CBX, n = 4; capsazepine, n = 8). (C) Schematic of the vector constructs. (D) Relative mRNA expression levels of TRPM3, TRPM7, and TRPM8 in U-87 MG cells after shRNA-mediated knockdown, normalized to shSC. (E) Fluorescence images showing mCherry, GFP, and merged signals in U-87 MG cells infected with shTRPM3-mCherry. White arrows indicate representative cells. Scale bar = 50 μm. (F) Representative ATP traces recorded from U-87 MG (upper left), U-373 MG (lower left), and patient-derived GBM (lower right) cells infected with scrambled shRNA (shSC) or shTRPM3 #1. Representative ATP traces recorded from U-87 MG (upper, right) cells infected with shSC or shTRPM3 #2. (G) Bar graph comparing ATP responses ( ΔF/F₀ ) in each cell line (U-87 MG infected shTRPM3 #1, n = 28; U-87 MG infected shTRPM3 #2, n = 14; U-373 MG infected shTRPM3 #1, n = 10; patient-derived GBM infected shTRPM3 #1, n = 14). (H) Representative ATP traces recorded from U-87 MG cells infected with shSC or shTRPM7 (left) and corresponding bar graph comparing ATP responses ( ΔF/F₀ ) between shSC – and shTRPM7-infected cells (right) (n = 20 per condition). (I) Representative ATP traces recorded from U-87 MG cells infected with shSC or shTRPM8 (left) and corresponding bar graph comparing ATP responses ( ΔF/F₀ ) between shSC – and shTRPM8-infected cells (right) (n = 10 per condition). Each dot represents ATP responses of an individual cell. Data are presented as mean ± SEM. (B, D) Ordinary one-way ANOVA (Multiple comparisons). (G) Multiple Mann-Whitney tests. (H, I) Two-tailed unpaired t-test. * p < 0.05, ** p < 0.01, **** p < 0.0001.

Article Snippet: The pharmacological agents, including 200 μM 2-APB (Tocris, #1224), 20 μM SKF-96365 hydrochloride (Tocris, #1147), 40 μM HC-030031 (Tocris, #2896), 100 μM quinine hydrochloride (Tocris, #4114), 1 μM carbenoxolone disodium (Tocris, #3096), and 10 μM capsazepine (Tocris, #0464), were dissolved in the external solution.

Techniques: Plasmid Preparation, Construct, Expressing, shRNA, Knockdown, Fluorescence, Infection, Derivative Assay, MANN-WHITNEY, Two Tailed Test

Change of Ca5 fluorescence induced by PUFAs and their endocannabinoid related metabolites in HEK-293 EV and TRPV1 expressing cells. Elevations of [Ca] i in response to PUFAs and their endocannabinoid-related molecules in HEK-293 EV cells, or cells expressing TRPV1. Drugs were tested at 10 µM or up to 30 µM, changes in [Ca] i are expressed as percentage of predrug baseline and were determined as outlined in the Methods. An unpaired t-test was conducted to compare their response in HEK-293 EV cell with that of HEK-293 TRPV1 expressing cells. An asterisk (*) indicates P < 0.05 compared to EV cells. The maximal percentage change in Ca5 fluorescence (E max ± SEM) and potency ( p EC 50 ) for PUFAs and their derivatives in HEK-293 TRPV1 cells were reported either for the highest tested concentration (30 µM) or derived from concentration-response curves (DHEA, AEA and NADA). Capsaicin is included for comparison. All values represent the mean ± SEM of at least 6 determinations. “n.d” signifies “not determined”, while “-” denotes “not tested.”

Journal: PeerJ

Article Title: Polyunsaturated fatty acids and their endocannabinoid-related metabolites activity at human TRPV1 and TRPA1 ion channels expressed in HEK-293 cells

doi: 10.7717/peerj.19125

Figure Lengend Snippet: Change of Ca5 fluorescence induced by PUFAs and their endocannabinoid related metabolites in HEK-293 EV and TRPV1 expressing cells. Elevations of [Ca] i in response to PUFAs and their endocannabinoid-related molecules in HEK-293 EV cells, or cells expressing TRPV1. Drugs were tested at 10 µM or up to 30 µM, changes in [Ca] i are expressed as percentage of predrug baseline and were determined as outlined in the Methods. An unpaired t-test was conducted to compare their response in HEK-293 EV cell with that of HEK-293 TRPV1 expressing cells. An asterisk (*) indicates P < 0.05 compared to EV cells. The maximal percentage change in Ca5 fluorescence (E max ± SEM) and potency ( p EC 50 ) for PUFAs and their derivatives in HEK-293 TRPV1 cells were reported either for the highest tested concentration (30 µM) or derived from concentration-response curves (DHEA, AEA and NADA). Capsaicin is included for comparison. All values represent the mean ± SEM of at least 6 determinations. “n.d” signifies “not determined”, while “-” denotes “not tested.”

Article Snippet: Capsaicin, the canonical activator of TRPV1 (Caps) was obtained from Tocris Bioscience, Bristol (# 404-86-4) and the TRPV1 antagonist capsazepine was from Merck, USA (# 138977-28-3).

Techniques: Fluorescence, Expressing, Concentration Assay, Derivative Assay, Comparison

(A) Concentration-response curves of PUFAs in HEK-293 TRPV1 expressing cells. The curves of DHA, γ-LA and in 9:3:1 ratio are overlapping; (B) effects of pre-incubation with PUFAs on responses to capsaicin in HEK-293 TRPV1 expressing cells. PUFAs or capsazepine (CAPZ) (10 µM each) were added to the cells for 5 min then capsaicin (10 nM) was added. Changes in [Ca] i are expressed as percentage of the pre-drug baseline. The black circles represent the response to first drug in individual experiments, while the pink circles correspond to the response to subsequent capsaicin addition. Two-way ANOVA with Dunnett’s multiple comparisons were used to analyze the response to capsaicin after pre-application of each PUFA and CAPZ, compared to capsaicin alone (HBSS served as a control in place of PUFAs and CAPZ). A significant difference ( P < 0.0001) was observed only for capsaicin pre-treated with CAPZ, while no significant differences were detected for the other conditions.

Journal: PeerJ

Article Title: Polyunsaturated fatty acids and their endocannabinoid-related metabolites activity at human TRPV1 and TRPA1 ion channels expressed in HEK-293 cells

doi: 10.7717/peerj.19125

Figure Lengend Snippet: (A) Concentration-response curves of PUFAs in HEK-293 TRPV1 expressing cells. The curves of DHA, γ-LA and in 9:3:1 ratio are overlapping; (B) effects of pre-incubation with PUFAs on responses to capsaicin in HEK-293 TRPV1 expressing cells. PUFAs or capsazepine (CAPZ) (10 µM each) were added to the cells for 5 min then capsaicin (10 nM) was added. Changes in [Ca] i are expressed as percentage of the pre-drug baseline. The black circles represent the response to first drug in individual experiments, while the pink circles correspond to the response to subsequent capsaicin addition. Two-way ANOVA with Dunnett’s multiple comparisons were used to analyze the response to capsaicin after pre-application of each PUFA and CAPZ, compared to capsaicin alone (HBSS served as a control in place of PUFAs and CAPZ). A significant difference ( P < 0.0001) was observed only for capsaicin pre-treated with CAPZ, while no significant differences were detected for the other conditions.

Techniques: Concentration Assay, Expressing, Incubation, Control

(A) Response of HEK-293 TRPV1 expressing cells for PMA at various concentration. PMA were added to the cells at different concentrations for 5 min then capsaicin was added at 10 nM. One-way ANOVA with Dunnett’s multiple comparisons shows that 300 nM PMA potentiation significantly enhances the capsaicin response ( P = 0.0098), while 100 nM and 10 nM PMA do not show a significant effect compared to capsaicin alone. (B) Traces of capsaicin and (C) Concentration response curves of capsaicin with and without PMA in HEK-293 TRPV1 expressing cells. Drugs were added for the duration of the bar; (D) The effects of PUFAs after potentiation of TRPV1 by PMA. The cells were pretreated with PMA (100 nM) for 5 min then each PUFA (10 µM) and capsaicin (10 nM) was added. Changes in [Ca] i are expressed as percentage of the pre-drug baseline, with the response to PMA alone at 5 min subtracted. The black circles represent the response of PUFAs without PMA pretreatment while the pink circles represent the response of PUFAs after PMA potentiation. Two-way ANOVA with Sidák’s multiple comparisons test revealed significant differences in the responses of EPA, DHA, and capsaicin before and after PMA potentiation, with p -values of 0.0396, 0.0059, and <0.0001, respectively.

Journal: PeerJ

Article Title: Polyunsaturated fatty acids and their endocannabinoid-related metabolites activity at human TRPV1 and TRPA1 ion channels expressed in HEK-293 cells

doi: 10.7717/peerj.19125

Figure Lengend Snippet: (A) Response of HEK-293 TRPV1 expressing cells for PMA at various concentration. PMA were added to the cells at different concentrations for 5 min then capsaicin was added at 10 nM. One-way ANOVA with Dunnett’s multiple comparisons shows that 300 nM PMA potentiation significantly enhances the capsaicin response ( P = 0.0098), while 100 nM and 10 nM PMA do not show a significant effect compared to capsaicin alone. (B) Traces of capsaicin and (C) Concentration response curves of capsaicin with and without PMA in HEK-293 TRPV1 expressing cells. Drugs were added for the duration of the bar; (D) The effects of PUFAs after potentiation of TRPV1 by PMA. The cells were pretreated with PMA (100 nM) for 5 min then each PUFA (10 µM) and capsaicin (10 nM) was added. Changes in [Ca] i are expressed as percentage of the pre-drug baseline, with the response to PMA alone at 5 min subtracted. The black circles represent the response of PUFAs without PMA pretreatment while the pink circles represent the response of PUFAs after PMA potentiation. Two-way ANOVA with Sidák’s multiple comparisons test revealed significant differences in the responses of EPA, DHA, and capsaicin before and after PMA potentiation, with p -values of 0.0396, 0.0059, and <0.0001, respectively.

Techniques: Expressing, Concentration Assay

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trpv1 blocker capsazepine (Tocris)

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1) Product Images from "Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain."

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