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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.
SA-13353 is a potent agonist of the TRPV1 receptor, known for its cardioprotective effects. This compound is instrumental in the study of cardiovascular diseases, facilitating research into mechanisms of cardiac protection and potential therapeutic interventions. Its ability to modulate TRPV1 activity makes it a valuable tool for investigating the role of this receptor in cardiovascular health.
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AS1928370 is a selective antagonist of the TRPV1 ion channel, demonstrating the ability to inhibit ligand-induced activation in vivo. This CNS-penetrant compound is particularly valuable for studying mechanisms underlying neuropathic pain. Its application in research offers insights into pain modulation and potential therapeutic strategies for pain management.
4-Methyl-2-(1-piperidinyl)-quinoline-d10 is a deuterated analogue of ML204, functioning as a selective inhibitor of the TRPC4 and TRPC5 ion channels. This compound exhibits a significant 19-fold selectivity over TRPC6 and has minimal impact on other TRP channels, as well as voltage-gated sodium, potassium, and calcium channels. It is a valuable tool for investigating TRPC channel functions and their roles in various biological processes.
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TRPV1 antagonist 5 is a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. This compound demonstrates potent inhibitory activity against TRPV1, making it a valuable tool for studies focused on pain signaling and thermoregulation. Research applications include investigating nociceptive pathways and exploring therapeutic potential for inflammatory pain relief.
TRPV1 agonist-1 is a potent agonist of the transient receptor potential vanilloid 1 (TRPV1) channel, exhibiting EC50 values of 4.5 nM and 0.57 nM for human and rat TRPV1, respectively. This compound is effective in enhancing swallowing function in preclinical rat models, making it valuable for investigating dysphagia and related disorders. Its non-irritating profile allows for potential applications in functional studies involving TRPV1 modulation.
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JYL-273 analog-1 is a potent agonist of the transient receptor potential vanilloid 1 (TRPV1) ion channel, exhibiting a Ki value of 10.8 nM. This compound demonstrates significant analgesic activity, with an ED50 of 1.0 mg/kg in the PBQ-induced writhing test. JYL-273 analog-1 is suitable for investigations into pain mechanisms and the development of analgesic therapies.
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AMG8788 is a selective, orally active antagonist of the transient receptor potential melastatin 8 (TRPM8), exhibiting an IC50 of 63.2 nM. This compound demonstrates significant inhibitory activity on TRPM8, making it valuable for studying sensory perception, pain pathways, and thermoregulation. It serves as an important tool for research into conditions associated with TRPM8 modulation, including neuropathic pain and cold sensitivity.
TRPC5-IN-2 is a selective inhibitor of the transient receptor potential cation channel 5 (TRPC5), known for its role in calcium ion influx and various physiological processes. This compound has demonstrated significant inhibitory activity against TRPC5, making it valuable for research into calcium signaling and its implications in neurological disorders, cardiovascular diseases, and gene regulation. TRPC5-IN-2 is essential for studies aimed at elucidating the functional roles of TRPC5 and exploring potential therapeutic interventions.
TRPM5 agonist-1 is a potent TRPM5 agonist with a pEC50 of 8.1, demonstrating strong selectivity over related cation channels such as TRPM8, TRPV1, TRPV4, TRPA1, and TRPM4. This compound elicits a stimulatory effect on gastrointestinal transit in mouse models, making it valuable for studies focused on enhancing gastric motility. TRPM5 agonist-1 is suitable for research exploring the roles of TRPM5 in gastrointestinal physiology and motility regulation.
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AMG9678 is a selective, orally active antagonist of the transient receptor potential melastatin 8 (TRPM8) channel, exhibiting a potent inhibitory effect with an IC50 value of 31.2 nM. This compound is utilized in research focused on pain modulation, thermosensation, and neurogenic inflammation, providing insights into the role of TRPM8 in various physiological and pathological processes. Its specificity and potency make it a valuable tool for investigating TRPM8-related biological pathways.
TRPV4/TRPA1-IN-1 is a selective inhibitor of the TRPV4 and TRPA1 channels, effectively blocking calcium influx mediated by these targets. This compound demonstrates significant efficacy in reducing pain behaviors in mouse models, particularly in trigeminal stimulation and acute pancreatitis contexts. TRPV4/TRPA1-IN-1 is valuable for research focused on pain modulation and inflammation associated with acute pancreatitis.
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JNJ-38893777 is a selective antagonist of the transient receptor potential vanilloid type 1 (TRPV1) channel. By inhibiting neuronal hyperactivation, JNJ-38893777 effectively reduces inflammatory hyperalgesia, making it a valuable tool for studies focused on migraine headaches, as well as neuropathic and inflammatory pain research. Its oral activity further enhances its potential in pharmacological applications targeting pain modulation.
TRPV1 activator-1 is a capsaicin analog with a modified neck structure that specifically interacts with the T551 residue of the TRPV1 receptor. This compound is known for its ability to activate TRPV1, contributing to research on pain sensation and nociception. Its unique properties make it a valuable tool for studying the physiological and pharmacological aspects of TRPV1-mediated pathways in various pain-related studies.
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TRPV1 activator-2 is a capsaicin analog that specifically targets the TRPV1 ion channel, enhancing its activity in response to thermal and chemical stimuli. This compound is utilized in research to study pain signaling pathways, neuroinflammation, and the physiological effects of TRPV1 modulation. Its precise interactions with channel residues at the lipid-water interface contribute to a better understanding of TRPV1's role in nociception and potential therapeutic applications.
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Synonyms: KR 25018
Davasaicin is a derivative of capsaicin and functions as an orally active analgesic agent. It is primarily used for the management of pain through its interaction with TRPV1 receptors, leading to altered pain signaling pathways. This compound serves as a valuable tool for research focused on pain mechanisms and potential therapeutic interventions in acute and chronic pain conditions.
Synonyms: (E/Z)-Farnesyl diphosphate
(E/Z)-Farnesyl pyrophosphate is a 15-carbon isoprenoid that acts as a TRPM2 agonist, facilitating ion influx through the channel. As a critical metabolic intermediate of the mevalonate pathway, it plays a significant role in cholesterol synthesis, ubiquinones synthesis, and protein farnesylation. This compound is essential for research in cellular signaling and lipid metabolism, providing insights into various biological processes and potential therapeutic targets.
DFL23448 is a selective antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. It demonstrates potent inhibition with IC50 values of 10 nM and 21 nM in human embryonic kidney 293 cells stimulated by Cooling Agent 10 or cold exposure. DFL23448 exhibits minimal activity against other transient receptor potential channels, such as TRPV1, TRPA1, and TRPV4, as well as various G protein-coupled receptors. This compound has potential applications in modifying bladder function and alleviating bladder overactivity in in vivo models.
Synonyms: DuP 996 dihydrochloride
Linopirdine dihydrochloride is an agonist of the capsaicin receptor TRPV1, which plays a key role in nociception. This compound enhances intracellular calcium levels in HEK293 cells, leading to increased excitatory responses in mammalian nociceptors. Linopirdine dihydrochloride is valuable for research applications focused on pain mechanisms and sensory neuron function.
JYL-273 is a potent TRPV1 agonist, exhibiting an IC50 of 361 nM in CHO-TRPV1 cell lines. This compound is useful for studying pain mechanisms and sensory neuron activation, making it a valuable tool in pain research and neurobiology. Its ability to selectively activate TRPV1 can aid in the investigation of pain pathways and the development of analgesic therapies.
Synonyms: Murraxocin
Murpanicin is a coumarin compound that functions as a selective inhibitor of the thermosensitive transient receptor potential vanilloid 2 (TRPV2) channel. Its potent anti-inflammatory properties make it a valuable tool for studying inflammation pathways, while its insecticidal effects allow for exploration in entomological research. This compound offers potential applications in the development of therapeutic agents targeting TRPV2-mediated processes.
SAR-115740 is a TRPV1 antagonist that selectively inhibits the transient receptor potential vanilloid 1 channel. This compound has demonstrated developmental toxicity in H9 cell assays, highlighting its potential impact on cellular differentiation and viability. SAR-115740 is valuable for investigating inflammatory conditions and neurological disorders, contributing to research aimed at understanding pain mechanisms and developing therapeutic strategies.
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Palvanil is a potent TRPV1 desensitizing agent, acting as an analogue of Capsaicin. It exhibits significant anti-nociceptive and anti-inflammatory properties, making it a valuable tool in pain research. Palvanil's mechanism of action provides insights into the modulation of TRPV1 receptor activity, facilitating studies on pain and inflammatory pathways.
GRC-6211 is a selective antagonist of the TRPV1 receptor, demonstrated to be orally active. This compound exhibits significant anti-inflammatory effects, making it a valuable tool for research applications in pain modulation and inflammatory disease studies.
AZ12099548 is a selective antagonist of the TRPV1 receptor, which plays a critical role in pain and sensory perception. This compound effectively inhibits calcium mobilization induced by both capsaicin and low pH, making it a valuable tool for research into pain mechanisms and sensory disorders. Its utility in studying TRPV1-related pathways facilitates investigations into potential therapeutic strategies for inflammatory and neuropathic pain conditions.
TRPC5-IN-4 is a potent inhibitor of the TRPC5 channel, with an IC50 value of 14.07 nM for TRPC5 and 65 nM for TRPC4. This compound demonstrates minimal cytotoxicity, exhibiting no detrimental effects on liver and kidney cells. TRPC5-IN-4 is particularly valuable for investigating mechanisms underlying chronic kidney disease (CKD) and holds potential for supportive research in this area.
