TRPV

Vanilloids are a group of compounds, structurally related to capsaicin, thought to exert their actions via vanilloid receptors. The vanilloid receptor family (TRPV) is a member of the transient receptor potential (TRP) superfamily of ion channels, and have six members (TRPV1-6).

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
1116 AM 404
Vanilloid receptor agonist. Also anandamide transport inhibitor
1339 Anandamide
Endogenous CB and TRPV1 receptor agonist
1017 Anandamide (in Tocrisolve™ 100)
Endogenous CB and TRPV1 receptor agonist (in water-soluble emulsion)
1354 Arvanil
Potent TRPV1 (VR1) and CB1 agonist/anandamide transport inhibitor
0462 (E)-Capsaicin
Prototypic vanilloid receptor agonist
1556 6'-Iodoresiniferatoxin
High affinity TRPV1 agonist/partial agonist
1568 NADA
Endogenous TRPV1 agonist. Also CB1 agonist
1641 OLDA
Potent, selective endogenous TRPV1 agonist
0934 Olvanil
Potent vanilloid receptor agonist
1466 PPAHV
Non-pungent vanilloid receptor agonist
1137 Resiniferatoxin
Potent vanilloid receptor agonist
3745 RN 1747
Selective TRPV4 agonist

Antagonists

Cat No Product Name / Activity
5781 A 425619
Potent TRPV1 antagonist
4319 A 784168
Potent and selective TRPV1 antagonist
4330 AMG 21629
Potent and selective TRPV1 antagonist
5995 AMG 517
Potent TRPV1 antagonist
2316 AMG 9810
Potent and selective, competitive antagonist of TRPV1
2836 Arachidonyl serotonin
Dual FAAH inhibitor/TRPV1 antagonist
3875 BCTC
TRPV1 antagonist
0464 Capsazepine
Vanilloid receptor antagonist; also activator of ENaCδ
5106 GSK 2193874
Potent and selective TRPV4 antagonist; orally active
4100 HC 067047
Potent and selective TRPV4 antagonist
1975 6-Iodonordihydrocapsaicin
Potent, competitive vanilloid receptor antagonist
1362 5'-Iodoresiniferatoxin
Potent, silent TRPV1 antagonist
3361 JNJ 17203212
Reversible, competitive and potent TRPV1 antagonist
1577 L-R4W2
TRPV1 antagonist peptide
3746 RN 1734
Selective TRPV4 antagonist
5678 RN 9893 hydrochloride
Potent and selective TRPV4 antagonist
1439 Ruthenium Red
Blocks capsaicin-activated cation channels
1615 SB 366791
Potent, selective, competitive TRPV1 antagonist
3265 SB 452533
Potent TRPV1 receptor antagonist
4729 α-Spinasterol
TRPV1 antagonist; active in vivo
1098 Tranilast
Antiallergic; inhibits TRPV2-mediated responses

Modulators

Cat No Product Name / Activity
5246 MRS 1477
TRPV1 positive allosteric modulator

Activators

Cat No Product Name / Activity
4876 Eact
TRPV1 channel activator; also TMEM16A activator

Ligand-sets

Cat No Product Name / Activity
2181 Vanilloid TRPV1 Receptor Tocriset™
Selection of 5 vanilloid TRPV1 receptor ligands (Cat. Nos. 0462, 0934, 1137, 0464 and 1615)

Other

Cat No Product Name / Activity
5464 AC 4
Photoswitchable TRPV1 channel blocker
4104 MM-22
Biotinylated anandamide analog; blocks anandamide uptake
2203 PALDA
Endogenous lipid; potentiates effects of endovanilloids at TRPV1 receptors
2204 STEARDA
Endogenous lipid, active in vivo. Enhances effects of endovanilloids at TRPV1 receptors
1684 Tocrisolve™ 100
Water-soluble emulsion; negative control for reagents in TocrisolveTM 100

Vanilloids are a group of compounds, structurally related to capsaicin, thought to exert their actions via vanilloid receptors. The vanilloid receptor family (TRPV) is a member of the transient receptor potential (TRP) superfamily of ion channels, and six members (TRPV1-6) have so far been identified.

The six vanilloid receptor members have been divided into four groups on the basis of structure and function: TRPV1/2, TRPV3, TRPV4 and TRPV5/6. TRPV1-4 are thermosensitive, non-selective cation channels that exist as tetrameric complexes. They are activated by a range of stimuli including heat, protons, lipids and changes in osmolarity or pressure. TRPV5-6 are calcium selective channels that are involved in the absorption and reabsorption of calcium across intestinal and renal epithelia.

It has been proposed that cannabinoids are endogenous ligands for vanilloid receptors. Furthermore, adenosine has been shown to be an endogenous TRPV1 ligand and TRPV4 is activated by anandamide and arachidonic acid (Cat. No. 2756).

External sources of pharmacological information for TRPV :

Literature for TRPV

Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

TRPV Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
TRPV1 Human TRPV1 NM_018727 Q8NER1
Mouse Trpv1 NM_001001445 Q704Y3
Rat Trpv1 NM_031982 O35433
TRPV2 Human TRPV2 NM_016113 Q9Y5S1
Mouse Trpv2 NM_011706 Q9WTR1
Rat Trpv2 NM_017207 Q9WUD2
TRPV3 Human TRPV3 NM_145068 Q8NET8
Mouse Trvp3 NM_145099 Q8K424
Rat Trpv3 NM_001025757 Q4QYD9
TRPV4 Human TRPV4 NM_021625 Q96Q92
Mouse Trpv4 NM_022017 Q9EPK8
Rat Trpv4 NM_023970 Q9ERZ8
TRPV5 Human TRPV5 NM_019841 Q9NQA5
Mouse Trpv5 NM_001007572 P69744
Rat Trpv5 NM_053787 Q9JIP0
TRPV6 Human TRPV6 NM_014274 Q9H1D0
Mouse Trpv6 NM_022413 Q91WD2
Rat Trpv6 NM_053686 Q9R186

TRPV Pharmacological Data

Receptor
(other names)
TRPV1
VR1, OTRPC1, Vanilloid/capsaicin receptor
TRPV2
VRL-1, OTRPC2, GRC
TRPV3
VRL-3
TRPV4
VRL-2, OTRPC4, VR-OAC, TRP12
TRPV5
OTRPC3, ECaC, ECaC1, CaT2
TRPV6
ECaC2, CaT1, CaT-L
Description Vanilloid receptor, noxious thermosensor, non-selective cation channel Noxious heat, noxious thermosensor, non-selective cation channel Warmth sensor, moderately selective Ca2+ channel Osmosensor, moderately selective Ca2+ channel Highly selective Ca2+ channel Highly selective Ca2+ channel
Receptor distribution Dorsal root and trigeminal ganglia, brain, spinal cord, pancreas, skin epithelial, bladder Dorsal root and trigeminal ganglia, brain, spinal cord, spleen, lung, mast cells, vascular smooth muscle Brain (cortex, thalamus), skin, hair follicles, tongue, stomach, spinal cord, superior clavicular, dorsal root and trigeminal ganglia Brain, liver, kidney, adipose tissue, heart, testis, salivary gland, trachea Intestine, kidney, placenta, brain Kidney, intestine
Tissue Function Pain sensation, vasodilation Thermal pain sensation, mast cell function Putative warm sensation Osmolarity sensing with thermal modulation Active Ca+ (re)absorption Active Ca2+ (re)absorption
Key Activators Capsaicin (0462)
Resiniferatoxin (1137)
Anandamide (1339)
Olvanil (0934)
Heat (threshold ~ 43oC)
Protons
Ethanol
Noxious heat (threshold =52oC)
IGF-1
Increasing temperature (~35oC) Reduced osmolarity None (constitutively active) None (constitutively active)
Antagonists Capsazepine (0464)
5'-Iodoresiniferatoxin (1362)
Ruthenium red (1439)
JNJ 17203212 (3361)
AMG 9810 (2316)
PIP2
Ruthenium red (1439)
SKF 963365 (1147)
La3+
Ruthenium red (1439) Ruthenium red (1439) Ruthenium red (1439)
La3+
Ruthenium red (1439)
La3+

References

Gunthorpe et al (2002) The diversity in the vanilloid (TRPV) receptor family of ion channels. TiPS 23 183. Clapham et al (2003) International Union of Pharmacology. XLIII. Compendium of voltage-gated ion channels; transient receptor potential channels. Pharmacol.Rev. 55 591. Alexander et al (2004) Guide to receptors and channels. Br.J.Pharmacol. 141 S89.