| I9281 | | 5′-Iodoresiniferatoxin solid | Vanilloid receptor antagonist. | |
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| I7033 | | 6′-Iodoresiniferatoxin amorphous semi-solid | VR1 vanilloid receptor partial agonist. | |
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| I0909 | | 6-Iodonordihydrocapsaicin ≥98% (HPLC), solid | TRPV1 (V1) vanilloid receptor antagonist. | |
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| A2731 | | AMG 9810 ≥98% (HPLC), powder | AMG 9810 is a potent, non-vanilloid, antagonist of the TRPV1 receptor. IC50 = 17 nM. | |
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| SML0103 | | AMTB is a TRPM8-selective antagonist with no cross reactivity to TRPV1 or 4. The pIC50 of icilin activation of TRPM8 is 6.23 i.v. administration of AMTB reduced the frequency of rhythmic contractions in volume-loaded bladder and inhibited blood pressure and visceromotor reflex responses to bladder distention. | |
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| M2028 | | Capsaicin ≥95%, from Capsicum sp. | Prototype vanilloid receptor agonist. Neurotoxin; activates sensory neurons that give rise to unmyelinated C-fibers, many of which contain substance P. Topical application desensitizes the sensory nerve endings giving a paradoxical antinociceptive effect; systemic administration can be neurotoxic to capsaicin-sensitive cells, especially in newborn animals. | |
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| C191 | | Capsazepine ≥98% (HPLC), solid | Capsazepine is a specific vanilloid receptor antagonist; synthetic analog of capsaicin. | |
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| M1022 | | Dihydrocapsaicin from Capsicum sp., ~90% | VR1 vanilloid receptor agonist. | |
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| G0798 | | GSK1016790A ≥98% (HPLC) | GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014). | |
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| SML0143 | | HC-067047 is a potent, selective inhibitor of hTRPV4. The compound inhibits human, rat and mouse TRPV4 with IC50 values of 48, 133 and 17 nM, respectively. HC-067047 does not inhibit other TRPV isoforms at concentrations up to 5 μM. HC-067047 inhibits hERG channel and the menthol receptor TRPM8 with IC50 values of 370 and 780 nM, respectively. | |
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| I9532 | | Icilin ≥97% (HPLC), solid | Icilin is a potent agonist at the CMR1 cold- and menthol-sensitive receptor. | |
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| I1279 | | Isovelleral solid | Vanilloid receptor agonist. | |
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| J3580 | | JNJ 17203212 ≥98% (HPLC) | JNJ 17203212 is a reversible, competitive and potent TRPV1 antagonist that does not inhibit related TRP channels such as TRPV2, TRPV4, or TRPA1. Listed in BJP with IC50= 65 nM. TRPV1 channels are activated by heat, capsaicin and the endocannabinoid anandamide. Interest in TRPV1 antagonists in the transmission and modulation of pain. | |
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| O2139 | | N-Oleoyldopamine >98%, powder | N-Oleoyldopamine is an endogenous vanilloid; weak CB1 receptor ligand. | |
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| V9130 | | N-Vanillylnonanamide ≥97%, powder | | |
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| O2389 | | OMDM-1 ≥97% (HPLC), powder | Potent, selective inhibitor of anadamide cellular uptake with low affinity for CB1 and CB2 receptors, no activity at VR1 receptor or fatty acid amide hydrolase (FAAH); stable to enzymatic hydrolysis by rat brain homogenates. | |
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| O0257 | | Olvanil powder | Vanilloid receptor agonist | |
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| P9983 | | Phorbol 12,13-didecanoate 20-homovanillate ≥98% | Resiniferatoxin-type vanilloid phorbol ester with capsaicin-like selectivity for the vanilloid receptor. | |
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| P0234 | | Phorbol 12,13-dinonanoate 20-homovanillate | Resiniferatoxin-type vanilloid phorbol ester with capsaicin-like selectivity for the vanilloid receptor. | |
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| P266 | | Phorbol 12-phenylacetate 13-acetate 20-homovanillate solid | Vanilloid receptor agonist. | |
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| R0658 | | RN-1734 ≥98% (HPLC) | RN-1734 is a selective TRPV4 antagonist. | |
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| R8756 | | Resiniferatoxin from Euphorbia poisonii, ~95% | Potent VR1 vanilloid receptor agonist that has been used to label the vanilloid receptor in sensory ganglia; activates protein kinase C. Diterpene ester that is related to phorbol, but is not tumorigenic. | |
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| S0441 | | SB-366791 ≥98% (HPLC), powder | Vanilloid receptor-1 (TRPV1) antagonist. | |
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