Date published: 2025-12-18

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VR1 Activators

The chemical class of VR1 activators encompasses a diverse group of compounds that can either directly or indirectly modulate the activity of the vanilloid receptor 1 (VR1), also known as the transient receptor potential vanilloid 1 (TRPV1). VR1 is a non-selective cation channel predominantly expressed in sensory neurons, where it plays a crucial role in the detection of noxious stimuli, including heat and certain chemical irritants. The identified VR1 activators exhibit a range of mechanisms to influence the activation of this ion channel. Direct activators of VR1 include capsaicin, resiniferatoxin, and olvanil. Capsaicin, found in chili peppers, directly binds to VR1, leading to channel opening and the sensation of heat or pain. Resiniferatoxin, a potent analog of capsaicin, similarly activates VR1 by binding to its ligand-binding pocket. Olvanil, a synthetic vanilloid compound, mimics capsaicin's structure and directly activates VR1, inducing neuronal excitation through cation influx, particularly calcium ions. Indirect activators of VR1 involve compounds such as 2-APB, anandamide, and probenecid. 2-APB indirectly activates VR1 by modulating intracellular calcium levels. It inhibits inositol trisphosphate receptors (IP3Rs), leading to increased cytoplasmic calcium concentrations, which sensitize VR1 channels. Anandamide, an endogenous cannabinoid, indirectly activates VR1 by interacting with cannabinoid receptors, resulting in decreased cyclic AMP levels and enhanced VR1 response. Probenecid indirectly activates VR1 by inhibiting anion channels, causing membrane depolarization and subsequent VR1 activation. Further indirect activators include arachidonic acid, bradykinin, lysophosphatidic acid (LPA), and GSK1016790A. Arachidonic acid indirectly activates VR1 by acting as a substrate for lipoxygenases, producing leukotrienes that sensitize VR1 channels. Bradykinin activates VR1 indirectly through B2 receptor (B2R) signaling, involving phospholipase C (PLC) activation and intracellular calcium release. LPA activates VR1 indirectly via LPA receptor signaling, leading to increased intracellular calcium and sensitization of VR1. GSK1016790A indirectly influences VR1 activation by activating TRPV4 channels, modulating intracellular calcium levels and affecting VR1-regulated pathways.

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Items 1 to 10 of 18 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Capsaicin

404-86-4sc-3577
sc-3577C
sc-3577D
sc-3577A
50 mg
250 mg
500 mg
1 g
$94.00
$173.00
$255.00
$423.00
26
(1)

Capsaicin acts as a potent agonist of the TRPV1 receptor, engaging in specific hydrogen bonding and hydrophobic interactions that facilitate its activation. Its unique structure allows for a high degree of conformational adaptability, which is crucial for effective receptor binding. The compound's lipophilicity enhances its diffusion across cellular membranes, while its interaction kinetics reveal a rapid onset of receptor activation, leading to distinct sensory signaling pathways.

N-Oleoyldopamine (OLDA)

105955-11-1sc-201456
sc-201456A
5 mg
25 mg
$75.00
$367.00
(0)

N-Oleoyldopamine (OLDA) is a selective modulator of the TRPV1 receptor, characterized by its unique fatty acid chain that enhances membrane fluidity and receptor accessibility. Its molecular structure promotes specific van der Waals interactions, facilitating a stable binding conformation. OLDA exhibits distinct reaction kinetics, with a gradual activation profile that influences downstream signaling pathways. This compound's amphipathic nature allows it to interact with lipid bilayers, impacting cellular responses.

AM-404

198022-70-7sc-200363B
sc-200363
sc-200363C
sc-200363A
5 mg
10 mg
25 mg
50 mg
$46.00
$65.00
$147.00
$242.00
(0)

AM-404 is a potent modulator of the TRPV1 receptor, distinguished by its ability to disrupt lipid bilayer integrity, leading to altered receptor dynamics. Its unique structure enables strong hydrogen bonding and hydrophobic interactions, enhancing receptor affinity. The compound exhibits rapid kinetics, promoting swift receptor activation and subsequent signaling cascades. Additionally, AM-404's amphiphilic characteristics facilitate its integration into cellular membranes, influencing membrane potential and ion flux.

Oleylethanolamide

111-58-0sc-201400
sc-201400A
10 mg
50 mg
$88.00
$190.00
1
(1)

Oleylethanolamide acts as a selective modulator of the TRPV1 receptor, characterized by its unique fatty acid amide structure that promotes specific lipid interactions. This compound enhances receptor sensitivity through its ability to stabilize membrane microdomains, influencing receptor conformational states. Its hydrophobic tail allows for effective integration into lipid membranes, potentially altering membrane fluidity and impacting downstream signaling pathways. The compound's dynamic interactions contribute to its distinct regulatory role in cellular processes.

Evodiamine

518-17-2sc-201479
sc-201479A
20 mg
100 mg
$20.00
$71.00
2
(1)

Evodiamine is a potent modulator of the TRPV1 receptor, distinguished by its unique indole alkaloid structure that facilitates specific binding interactions. This compound engages in allosteric modulation, altering receptor dynamics and enhancing calcium ion influx. Its ability to interact with lipid bilayers influences membrane properties, potentially affecting receptor localization and activation. The intricate balance of hydrophilic and hydrophobic regions in Evodiamine contributes to its nuanced regulatory effects on sensory signaling pathways.

2-APB

524-95-8sc-201487
sc-201487A
20 mg
100 mg
$27.00
$52.00
37
(1)

2-APB is a selective modulator of the TRPV1 receptor, characterized by its ability to disrupt calcium signaling pathways. This compound exhibits unique interactions with the receptor's transmembrane domains, influencing ion channel gating and permeability. Its structural features allow for effective competition with endogenous ligands, altering receptor conformation. Additionally, 2-APB's amphipathic nature enables it to interact with cellular membranes, potentially impacting lipid dynamics and receptor clustering.

Nonivamide

2444-46-4sc-202735
sc-202735A
25 mg
100 mg
$20.00
$77.00
6
(0)

Nonivamide is a potent agonist of the TRPV1 receptor, known for its unique ability to induce receptor activation through specific hydrophobic interactions. Its molecular structure facilitates binding to the receptor's allosteric sites, enhancing ion flow and modulating thermal nociception pathways. The compound's lipophilic characteristics promote membrane integration, influencing receptor localization and clustering, which can alter cellular excitability and signaling cascades.

Dihydrocapsaicin

19408-84-5sc-202578
sc-202578A
10 mg
50 mg
$51.00
$153.00
1
(1)

Dihydrocapsaicin acts as a selective agonist for the TRPV1 receptor, engaging in unique hydrogen bonding and hydrophobic interactions that stabilize receptor conformation. Its structural features allow for enhanced receptor activation, influencing calcium ion influx and subsequent neuronal signaling. The compound's high lipophilicity aids in membrane penetration, potentially affecting receptor dynamics and distribution, thereby modulating sensory perception and pain pathways.

Olvanil

58493-49-5sc-201454
sc-201454A
5 mg
25 mg
$47.00
$201.00
1
(0)

Olvanil is a potent TRPV1 receptor agonist characterized by its unique molecular interactions that facilitate receptor activation. Its distinct hydrophobic regions promote effective binding, enhancing conformational changes within the receptor. This compound exhibits rapid kinetics in receptor engagement, leading to a swift influx of calcium ions. Additionally, its lipophilic nature enhances membrane affinity, influencing the spatial distribution of the receptor and modulating sensory signaling pathways.

12(S)-HPETE

71774-10-2sc-200961A
sc-200961
25 µg
50 µg
$153.00
$260.00
(0)

12(S)-HPETE is a bioactive lipid mediator that selectively interacts with the TRPV1 receptor, promoting its activation through specific hydrogen bonding and hydrophobic interactions. This compound is known for its role in modulating inflammatory responses, as it influences intracellular signaling cascades. Its unique structural features allow for rapid receptor binding and subsequent calcium ion mobilization, contributing to its role in sensory transduction and nociceptive signaling pathways.