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Transient receptor potential (TRP) channel modulators act on cation channels that sense heat, cold and irritants. The mammalian family has six subfamilies, including vanilloid (TRPV), ankyrin (TRPA), canonical (TRPC) and melastatin (TRPM) channels. TRP channels respond to temperature, touch, osmotic changes and plant-derived compounds, so they are often described as cellular sensors. Cloning of the capsaicin receptor TRPV1 in 1997 identified it as a heat-activated ion channel in pain-sensing neurons. AMG517 and SB-705498 are TRPV1 antagonists, while A 967079 blocks TRPA1 and optovin activates TRPA1 when exposed to light. Pyr10 inhibits TRPC3, and Pico145 inhibits channels formed by TRPC1, TRPC4 and TRPC5. The spider toxin peptide GsMTx4, an inhibitor of mechanosensitive channels, is also listed under Piezo Channel.
Evifacotrep is a potent antagonist of the transient receptor potential channel 5 (TRPC5) with an IC50 of ≤50 nM. This compound effectively inhibits TRPC5/TRPC4 activity, making it a valuable tool for investigating neurological diseases. Its selective mechanism of action allows for detailed study of TRPC channel involvement in various pathophysiological processes.
RN-9893 is a potent and selective antagonist of the TRPV4 receptor, exhibiting IC50 values of 320 nM, 420 nM, and 660 nM for mouse, human, and rat channels, respectively. This compound is valuable for research applications involving the modulation of TRPV4-mediated physiological processes. Its selective inhibition can aid in studies related to pain sensation, inflammation, and other TRPV4-associated diseases.
LY3526318 is a selective antagonist of the TRPA1 ion channel, with an IC50 of 5-6 μM. This compound effectively inhibits TRPA1-mediated pain signal transduction, demonstrating notable analgesic activity. LY3526318 is primarily utilized in research focused on chronic pain conditions, including diabetic peripheral neuropathy, chronic low back pain, and osteoarthritis-related pain.
SB 452533 is a potent and selective antagonist of the TRPV1 ion channel. It demonstrates a pKb of 7.8, indicating strong binding affinity and inhibitory activity. This compound is primarily utilized in research applications related to pain modulation and inflammation, offering insights into the role of TRPV1 in nociception and sensory neurons. SB 452533 is an essential tool for studying pain pathways and developing potential analgesic therapies.
Synonyms: SAF312; Vanilloid receptor antagonist 1
Libvatrep is a selective TRPV1 antagonist that inhibits the activity of the transient receptor potential vanilloid 1 channel. It exhibits significant anti-nociceptive effects, making it a valuable tool for research in pain modulation and sensory neuron signaling. This compound is useful in investigations of neurogenic inflammation and the potential treatment of chronic pain conditions.
GSK2220691 is a potent antagonist of the transient receptor potential vanilloid 4 (TRPV4) channel. This compound effectively inhibits pulmonary edema induced by GSK1016790 and reduces HCl-induced increases in key mediators such as vascular endothelial growth factor (VEGF), keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF). GSK2220691 serves as a valuable tool for investigating TRPV4-related pathways and therapeutic applications in respiratory disorders.
Oleoyl Serotonin is a TRPV1 antagonist, exhibiting an IC50 value of 2.57 μM for human TRPV1 receptors. This compound is implicated in the modulation of nociceptive pathways, making it a valuable tool for studies related to pain signaling and sensory transduction. Oleoyl Serotonin is suitable for research applications investigating inflammatory pain and potential therapeutic interventions targeting TRPV1.
TRPM8 Antagonist 3 is a selective antagonist targeting the Transient Receptor Potential Melastatin 8 (TRPM8) channel, exhibiting an IC50 value of 11 nM. This compound effectively inhibits TRPM8-mediated calcium influx, making it useful for studying nociceptive pathways and cold sensitivity. It has potential applications in research related to pain management, sensory biology, and neurobiology.
Synonyms: 3-O-Methyl estradiol; 17β-Estradiol 3-methyl ether; 3-Methoxyestradiol
Estradiol 3-methyl ether (EDME) is a potent antagonist of the TRPML1 ion channel and a microtubule depolymerizer. It exhibits remarkable selectivity, with IC50 values of 0.22 μM against TRPML1 and 3.8 μM against TRPML2, while showing no activity towards TRPML3. EDME disrupts cytoplasmic microtubule networks in mammalian cells with an EC50 of 9 μM. This compound operates independently of estrogen receptors to block autophagy, inhibit TFEB nuclear translocation, and reduce migration and invasion in triple-negative breast cancer cells, making it highly relevant for research in cancer biology.
ABT-102 is a potent and highly selective antagonist of the Transient Receptor Potential Vanilloid 1 (TRPV1) channel. This compound effectively elevates heat pain thresholds and diminishes the perception of pain in response to suprathreshold heat stimuli. ABT-102 has demonstrated efficacy in reducing nociceptive responses in various animal models, including those simulating inflammatory pain, bone cancer pain, postoperative pain, and osteoarthritis.
Voacangine is a selective antagonist of the TRPM8 channel, competitively inhibiting the binding of menthol (IC50=9 μM) and noncompetitively inhibiting icilin (IC50=7 μM). It is known to block capsaicin binding to TRPV1 (IC50=50 μM) while exhibiting agonistic effects on TRPA1 (EC50=8 μM). Voacangine effectively antagonizes chemical agonist-induced activation of TRPM8, with no impact on cold-induced activation, making it a valuable tool for studying sensory signaling pathways. This alkaloid is derived from the root bark of Voacanga africana, providing a natural source for research applications.
L-R4W2 is a potent antagonist of the vanilloid receptor 1 (VR1, TRPV1), exhibiting an IC50 of 0.1 μM. This compound demonstrates significant analgesic properties, making it a valuable tool in pain management research. L-R4W2 can be utilized to explore mechanisms of pain signaling and the therapeutic potential for treating pain-related disorders.
AMG 7905 is a selective antagonist of the transient receptor potential vanilloid type 1 (TRPV1), known for its role in mediating pain and thermoregulation. This compound effectively inhibits TRPV1 channel activation by capsaicin while enhancing channel activation by protons. AMG 7905 is employed in research focusing on pain modulation, thermogenesis inhibition, and the physiological responses to temperature changes.
(S)-ABT-102 is a selective TRPV1 antagonist with an IC50 of 123 nM. It exhibits significant analgesic activity, making it a valuable tool for exploring pain pathways. This compound is utilized in research applications focused on pain management and the study of nociception mechanisms.
TRPA1-IN-1 is a selective antagonist of the TRPA1 channel, exhibiting potent inhibitory effects on this target. This small molecule demonstrates oral bioavailability, making it suitable for in vivo studies. TRPA1-IN-1 is valuable for investigating the role of TRPA1 in pain signaling and inflammatory responses, contributing to research in neurobiology and pharmacology.
Synonyms: BHV-2100
Ponometrep is a potent antagonist of the transient receptor potential melastatin 3 (TRPM3) channel, exhibiting IC50 values in the range of 1-10 nM. This compound demonstrates significant analgesic activity, making it a valuable tool for the study of pain mechanisms and neurological disorders. Its specificity for TRPM3 allows researchers to explore potential therapeutic applications in related biological pathways.
V116517 is a potent orally active antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. It effectively inhibits capsaicin- and acid-induced currents in rat dorsal root ganglion neurons expressing native TRPV, with IC50 values of 423.2 nM for capsaicin and 180.3 nM for acid. This compound is valuable for research related to pain mechanisms and potential therapeutic interventions.
TRPV4 antagonist 4 is a selective TRPV4 antagonist with an IC50 value of 22.65 nM, effectively inhibiting TRPV4-mediated ion currents. This compound demonstrates protective effects in models of acute lung injury, making it a valuable tool for research focused on respiratory diseases and cellular calcium signaling. Its specificity for the TRPV4 channel highlights its potential in studying TRPV4-related physiological and pathological processes.
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AMG0347 is a potent antagonist of the transient receptor potential type V1 (TRPV1) channel. It effectively inhibits TRPV1 activation by heat (IC50 = 0.2 nM), protons (IC50 = 0.8 nM), and capsaicin (IC50 = 0.7 nM). This compound is useful for research applications related to nociception, pain pathways, and sensory neuron function.
JTS-653 is a potent and selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. It demonstrates significant efficacy in attenuating chronic pain that is resistant to non-steroidal anti-inflammatory medications. This compound is valuable for research into pain management and the mechanisms underlying TRPV1-related conditions.
6-Iodonordihydrocapsaicin is a selective antagonist of the TRPV1 receptor. It effectively inhibits TRPV1-mediated responses, such as capsaicin-induced ion currents in dorsal root ganglion neurons and the distension-induced firing of jejunal spinal afferent fibers in murine models. This compound is valuable for research focused on visceral pain mechanisms and the exploration of anxiety disorders.
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TRPC Antagonist 1 is a potent antagonist of transient receptor potential channels, specifically targeting TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7, with IC50 values of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM, respectively. This compound exhibits significant anti-glioblastoma activity in vitro, effectively inhibiting the proliferation of U87 cell lines. It serves as a valuable tool for exploring the role of TRPC channels in various biological processes and disease models.
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CMP233 is a potent TRPM4 antagonist with an IC50 value of 0.15 μM. This compound is valuable in the study of neurodegenerative disorders, providing insights into the role of TRPM4 channels in various pathological conditions. Its high specificity and efficacy make it a key tool for researchers investigating TRPM4-mediated signaling pathways.
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AMG8163 is an orally active antagonist of the TRPV1 receptor. This compound effectively inhibits capsaicin-induced flinching in rat models, demonstrating significant anti-hyperalgesic properties across various pain models. AMG8163 serves as a valuable tool for research focused on pain mechanisms and potential therapeutic interventions for hyperalgesia.
RN-9893 hydrochloride is a potent antagonist of the transient receptor potential vanilloid 4 (TRPV4) channel, exhibiting IC50 values of 0.42 μM for human and 0.66 μM for rat TRPV4. This compound is valuable for research focused on TRPV4-related physiological processes and pathologies, including pain sensation and inflammatory responses. Its oral bioactivity makes it suitable for in vivo studies investigating the role of TRPV4 in various biological systems.
