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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.
MK6-83 is a potent agonist of TRPML1, exhibiting enhanced efficacy and activity. This compound exhibits potential for research into Mucolipidosis type IV, facilitating investigations into the physiological role of TRPML1 and its implications in related pathologies. Its use may contribute to a deeper understanding of lysosomal function and associated disorders.
Synonyms: NBA
TRPM4-IN-2 is a potent inhibitor of the transient receptor potential melastatin 4 (TRPM4) channel, exhibiting an IC50 value of 0.16 µM. This compound is particularly relevant in the study of prostate and colorectal cancers, providing valuable insights into TRPM4's role in tumor biology and potential therapeutic pathways. Its ability to modulate TRPM4 activity makes it a useful tool in cancer research and drug development.
Umbellulone is a potent TRPA1 channel activator derived from the leaves of Umbellularia californica. This compound selectively stimulates TRPA1 channels in peptidergic, nociceptive neurons, thereby activating the trigeminovascular system. Umbellulone is valuable for research applications focused on pain signaling pathways and the mechanisms underlying migraine and other pain-related disorders.
Synonyms: OLDA
N-Oleoyldopamine is an oral TRPV1 activator and 5-lipoxygenase (5-LOX) inhibitor that effectively crosses the blood-brain barrier. It stimulates histaminergic neurons in the tuberomammillary nucleus via a dopamine receptor mechanism, independent of TRPV1 and cannabinoid receptors. N-Oleoyldopamine enhances insulin release and promotes glucose-dependent insulinotropic polypeptide through a GPR119-dependent pathway, thus improving glucose tolerance. Additionally, it benefits cardiovascular health by mitigating left ventricular dysfunction and reducing myocardial infarction size through the release of substance P and calcitonin gene-related peptide. This compound is valuable for research into glycemic control and myocardial ischemia-reperfusion injury.
Synonyms: RvD2
Resolvin D2 is a potent TRPV1 and TRPA1 inhibitor with a primary mechanism targeting these transient receptor potential channels in primary sensory neurons. As a metabolite of docosahexaenoic acid (DHA), it exhibits significant anti-inflammatory and anti-infective properties, effectively regulating leukocyte function and controlling microbial sepsis. This compound's high potency and specificity make it a valuable tool in research focused on pain modulation and inflammatory responses.
Synonyms: CBA
TRPM4-IN-1 is a selective inhibitor of the TRPM4 ion channel, exhibiting an IC50 value of 1.5 μM. This compound is primarily utilized in studies related to cardiac diseases and prostate cancer, facilitating insights into the role of TRPM4 in these conditions. Its potency makes it a valuable tool for investigating the modulation of calcium signaling pathways in various biological contexts.
Synonyms: SYL1001 sodium
Tivanisiran sodium is a small interfering RNA (siRNA) that targets the mRNA of transient receptor potential vanilloid 1 (TRPV1). It is primarily utilized in the research of dry eye disease by effectively silencing TRPV1 expression, which is involved in pain and sensory signaling. This agent facilitates the exploration of TRPV1's role in ocular conditions, contributing to the development of potential therapeutic strategies for managing dry eye symptoms.
ASP7663 is a potent and selective agonist of the transient receptor potential ankyrin 1 (TRPA1) channel. Its pharmacological profile indicates significant biological activity in alleviating constipation and reducing abdominal pain. ASP7663 serves as a valuable tool for research into gastrointestinal disorders and the modulation of nociceptive pathways.
Moringin is a potent and selective natural agonist of the TRPA1 ion channel, exhibiting an EC50 value of 3.14 μM. It demonstrates minimal activation of vanilloid channels TRPV1, TRPV2, TRPV3, and TRPV4, as well as the cooling receptor TRPM8. Moringin is associated with various biological activities, including hypoglycemic, antimicrobial, anti-inflammatory, anticancer, and neuroprotective effects, making it valuable for research applications in these areas.
BTD is a selective activator of the transient receptor potential canonical 5 (TRPC5) channel, known for its roles in neuronal signaling. This compound facilitates the investigation of TRPC5-mediated pathways, making it a valuable tool for research into neurological diseases and related physiological processes. The modulation of TRPC5 activity by BTD can provide insights into therapeutic targets and mechanisms associated with neurodegenerative conditions.
SOR-C13 is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel implicated in malignancy and poor prognosis in breast cancer. This compound exhibits significant anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development.
PF-05105679 is a selective antagonist of the transient receptor potential melastatin 8 (TRPM8) channel, exhibiting an IC50 of 103 nM. This compound demonstrates promising biological activity in modulating cold-related pain pathways. It is suitable for research applications investigating the role of TRPM8 in nociception and pain management strategies.
Synonyms: NE-19550; N-Vanillyloleamide
Olvanil (NE-19550) is a potent agonist of the transient receptor potential vanilloid type 1 (TRPV1) receptor, exhibiting an EC50 of 0.7 nM. This compound demonstrates analgesic properties and is valuable for investigating pain pathways and inflammatory responses. It is suitable for research applications focused on nociception and related signaling mechanisms.
AP-18 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1), effectively blocking TRPA1 activation by 50 µM cinnamaldehyde with IC50 values of 3.1 µM for human and 4.5 µM for mouse TRPA1. This compound demonstrates significant analgesic properties, as it reverses complete Freund's adjuvant-induced mechanical hyperalgesia in murine models. Additionally, AP-18 significantly reduces AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 µM, making it a valuable tool for research into pain mechanisms and TRPA1-related pathways.
Synonyms: VPC4
VPC01091.4 is a potent TRPM7 inhibitor that effectively blocks TRPM7 current at low micromolar concentrations. This compound is capable of crossing the blood-brain barrier, making it suitable for neurological studies. Additionally, VPC01091.4 demonstrates significant anti-inflammatory properties, halting systemic inflammation in vivo, and can be utilized in research focused on inflammation and neuronal signaling pathways.
TRPV3 antagonist 74a is a selective and potent inhibitor of the transient receptor potential vanilloid 3 (TRPV3) channel. Exhibiting minimal activity against a broad range of other ion channels, this compound serves as a valuable tool for investigating the role of TRPV3 in various biological processes. Its specific antagonistic properties make TRPV3 antagonist 74a particularly useful in research focusing on neuropathic pain and related disorders.
Synonyms: PAC-14028
Asivatrep (PAC-14028) is a potent and selective antagonist of the transient receptor potential vanilloid type I (TRPV1) channel. This compound exhibits significant analgesic effects by blocking TRPV1, which is involved in the transmission of nociceptive signals. Asivatrep is primarily utilized in research related to pain management and neurobiology. Its selective inhibition offers a valuable tool for studying TRPV1-mediated pathways and their role in various physiological and pathological conditions.
BAY-390 is a selective TRPA1 inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent inhibitory activity with IC50 values of 16 nM for human TRPA1 (hTRPA1) FLIPR, 82 nM for hTRPA1 electrophysiology (Ephys), 63 nM for rat TRPA1 (rTRPA1) FLIPR, and 35 nM for rat dorsal root ganglion (DRG) Ephys. BAY-390 is suitable for investigating the role of TRPA1 in inflammation-related research.
Synonyms: GDC-6599
Nedizantrep is a potent inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel, demonstrating IC50 values of 5.3 nM in humans and varying efficacy across different species. This compound is utilized in research focused on neuropathic pain and respiratory conditions, including asthma and chronic cough. Its selective action on TRPA1 underscores its potential as a valuable tool for advancing studies aimed at understanding and treating these conditions.
D-3263 hydrochloride is a selective agonist of the transient receptor potential melastatin member 8 (TRPM8) channel. This compound exhibits key biological activity by modulating nociceptive signaling pathways, which are involved in pain perception and temperature regulation. It is primarily utilized in research related to pain management, sensory neuronal activity, and the physiological responses to cold stimuli.
Synonyms: TRPC6-IN-3
Apecotrep is a potent inhibitor of the transient receptor potential C6 (TRPC6) ion channel. This orally active compound effectively modulates intracellular calcium levels and influences membrane potential by regulating the flux of calcium and sodium ions. Apecotrep is particularly relevant for research involving the respiratory system, providing insights into the role of TRPC6 in various biological processes.
TRPV4 agonist-1 free base is a selective agonist of the transient receptor potential vanilloid 4 (TRPV4) channel, demonstrating an EC50 of 60 nM in human TRPV4 calcium assays. This compound induces calcium influx and is instrumental in studies focused on the physiological roles of TRPV4 in nociception, osmoregulation, and cellular mechanotransduction. Research applications include investigating the channel's involvement in pain pathways and potential therapeutic targets for related disorders.
Synonyms: (+)-trans-ML-SI3
(1S,2S)-ML-SI3 is a selective activator of the TRPML2 and TRPML3 isoforms, exhibiting EC50 values of 2.7 μM and 10.8 μM, respectively, while serving as a potent inhibitor of TRPML1 with an IC50 of 5.9 μM. This compound facilitates investigations into lysosomal ion channel functions, cellular ion homeostasis, and related signaling pathways. Its unique pharmacological profile makes it a valuable tool for researchers studying the role of TRPML channels in various biological processes.
Mesendogen is a selective TRPM6 inhibitor that plays a crucial role in the regulation of magnesium homeostasis. It enhances the differentiation of human embryonic stem cells (hESCs) and human induced pluripotent stem cells (hiPSCs) into mesodermal and definitive endoderm lineages. This compound is valuable for research focused on early embryonic development and the role of magnesium in cellular processes.
Podocarpic acid is a natural compound that serves as a TRP channel agonist, specifically activating the TRPA1 channel. This compound demonstrates significant biological activity in modulating sensory nerve pathways and has potential applications in pain research and neurobiology. Its unique pharmacological profile makes it a valuable tool for investigating TRP channel function and related therapeutic targets.
