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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.
Synonyms: WaTx
Wasabi Receptor Toxin is an activator of the TRPA1 ion channel, functioning at nanomolar concentrations (EC50). This cell-penetrating scorpion toxin enhances the open time of TRPA1 while concurrently reducing calcium permeability. Its application in research includes the investigation of thermal hypersensitivity and mechanical allodynia in animal models, without inducing neurogenic inflammation.
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OptoBI-1 is a photochromic agonist of the TRPC3 channel, functioning as a photopharmacological agent to modulate neuronal activity. This compound enables precise control of neuronal firing through light-induced conformational changes, facilitating studies in neural circuitry and synaptic transmission. OptoBI-1 is valuable for researchers investigating the role of TRPC3 in neurophysiology and related biological processes.
Synonyms: 18:3 NAE; α-Linolenoyl ethanolamide
N-Linolenoylethanolamine (18:3 NAE) is a TRPV1 agonist that functions as an endocannabinoid. This compound is known to modulate pain and inflammatory responses through its interaction with the transient receptor potential vanilloid 1. It is valuable in research applications focused on neurobiology, pain management, and the endocannabinoid system.
(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.
TRPV4 agonist-1 is a selective agonist of the transient receptor potential vanilloid 4 (TRPV4) channel, exhibiting an EC50 of 60 nM in human TRPV4 calcium assays. This compound is primarily utilized in research to investigate TRPV4-mediated pathways, including physiological functions like osmosensation and nociception. Its ability to activate TRPV4 makes it valuable for studying various biological processes and potential therapeutic applications related to TRP channels.
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.
18:0-PhoDAG is a photoswitchable diacylglycerol (DAG) that enables precise photoactivation of DAG-sensitive transient receptor potential (TRP) channels. This compound serves as a valuable tool in elucidating the signaling pathways associated with TRP channel activity in various biological systems. Its use in photopharmacology facilitates real-time studies of cellular responses to DAG modulation, enhancing understanding of cellular signal transduction phenomena.
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Methyl kakuol is a selective agonist of the transient receptor potential ankyrin 1 (TRPA1) channel, exhibiting an effective concentration (EC50) of 0.27 µM. This compound facilitates the activation of TRPA1, making it a valuable tool for research into sensory pathways and pain mechanisms. Its ability to modulate TRPA1 activity can aid in the exploration of neurophysiological responses and the development of therapeutic strategies targeting pain and inflammation.
Polygodial pyridazine is a TRPV1 agonist that exhibits a GI50 of 72 μM against MCF-7 cancer cell lines. This compound is a polygodial analogue that plays a crucial role in exploring the mechanisms of pain perception and inflammation. It is applicable for research focused on cancer biology and the modulation of sensory neuronal pathways.
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AAL-149 is a selective inhibitor of the TRPM7 ion channel, exhibiting an IC50 value of 1.081 μM. This compound demonstrates multimodal anti-inflammatory effects while avoiding interaction with sphingosine-1-phosphate (S1P) receptors. AAL-149 is a valuable tool for researchers investigating the role of TRPM7 in inflammation and related biological pathways.
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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.
AMG-8562 is a selective modulator of the TRPV1 ion channel, effectively inhibiting capsaicin activation while sparing heat-induced activation. This compound enhances TRPV1 activation at acidic pH levels and demonstrates significant analgesic properties by blocking capsaicin-induced flinching behaviors in various pain models. AMG-8562 has shown substantial efficacy in models of thermal hyperalgesia induced by complete Freund's adjuvant and skin incision, as well as in acetic acid-induced writhing assays, making it a valuable tool for pain research.
TRPM8 receptor agonist-1 is a selective agonist for the TRPM8 receptor, known for its ability to induce the inward flow of calcium, sodium, and other ions, resulting in cell membrane depolarization and subsequent action potential generation. This compound plays a crucial role in activating pathways associated with the swallowing reflex, making it valuable for research on oropharyngeal dysphagia and related conditions. Its activation of TRPM8 receptors positions it as a significant tool for exploring ion channel dynamics and therapeutic approaches in dysphagic disorders.
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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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TRPV4-KCa2.3 modulator 1 is a modulator that enhances the TRPV4-KCa2.3 protein complex, exhibiting significant antihypertensive activity. This compound promotes hyperpolarization and vasodilation in endothelial cells. Its ability to influence vascular responses makes it a valuable tool for investigating hypertension and related cardiovascular disorders in research settings.
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TRPM2-IN-1 is a selective inhibitor of the TRPM2 ion channel, which plays a critical role in calcium influx and cellular signaling. This compound has demonstrated significant neuroprotective effects and exhibits antistroke activity, making it a valuable tool in the study of ischemic stroke and related neurological disorders. Its capacity to modulate TRPM2 activity provides insight into potential therapeutic strategies for neurodegenerative conditions.
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HZS60 is a selective TRP channel inhibitor that demonstrates significant neuroprotective effects against cerebral ischemia. It effectively mitigates primary neuronal damage induced by NMDA and oxygen-glucose deprivation/reoxygenation. Additionally, HZS60 exhibits favorable pharmacokinetic properties and can reduce injury associated with cerebral ischemia-reperfusion. This compound serves as a promising candidate for research applications targeting ischemic stroke.
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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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Synonyms: Coniferyl (E)-8-methyl-6-nonenoate
Capsiconiate, a TRPV1 agonist, exhibits a potent efficacy with an EC50 of 3.2 μM. This compound serves as a valuable tool for investigating TRPV1-mediated conditions, including pain, inflammation, and epilepsy. Its ability to activate the TRPV1 receptor makes it significant in the study of related pathophysiological mechanisms and therapeutic interventions.
AMG 9090 is a partial agonist of the rat TRPA1 channel, exhibiting significant pharmacological activity in models of pain and inflammation. TRPA1 plays a critical role in detecting reactive compounds that induce pain responses in both humans and rodents. Notably, AMG 9090 demonstrates a distinct antagonistic effect on human TRPA1 activated by AITC and noxious cold, while functioning as a partial agonist in rat TRPA1. This profile highlights the compound’s potential utility as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory effects observed on TRPM8 channels.
TRPV1-IN-3 is a selective inhibitor of the transient receptor potential vanilloid 1 (TRPV1) channel, demonstrating significant antifibrotic activity in vitro with an IC50 of 0.51 μM. Its mechanism involves the modulation of fibrosis markers such as collagen I and α-SMA through inhibition of the TGF-β/Smads and MAPK signaling pathways. Research applications include studying idiopathic pulmonary fibrosis, where TRPV1-IN-3 has been shown to reduce collagen deposition in lung tissue, enhance alveolar structure, and increase survival rates in Bleomycin-induced pulmonary fibrosis models.
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