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TRPV1 Agonists and Antagonists / Related Products
You are here: Product Lines > Neurobiology > TRPVs [Vanilloid Receptors] / Related Products > Vanilloid Receptor [TRPV1] / Related Products > TRPV1 Agonists and Antagonists / Related Products
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ALX-550-394 Revised 17-Dec-04
JYL-1511
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SYNONYMS N-(4-tert-Butylbenzyl)-N'-[3-methoxy-4-(methyl-
sulfonylamino)benzyl]thiourea
PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-550-394-M001   1 mg 80.00 USD Add To Cart
ALX-550-394-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C21H29N3O3S2
MW: 435.6
CAS NUMBER: 623166-14-3
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, DMSO or other organic solvents; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent TRPV1 antagonist. RTX binding affinity (Ki=50.4nM), agonism (calcium influx; EC50=32.4nM) and antagonism (IC50=3.37nM).
Product Specific Literature References
High-affinity partial agonists of the vanilloid receptor: Y. Wang, et al.; Mol. Pharmacol. 64, 325 (2003) Abstract
 
 
ALX-300-149 Revised 11-Jul-08
Linoleylethanolamide
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SYNONYMS N-(2-Hydroxyethyl)-9Z,12Z-octadecadienamide
LEA
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Endocannabinoids
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ALX-300-149-M005   5 mg 57.00 USD Add To Cart
Product Specification
FORMULA: C20H37NO2
MW: 323.5
CAS NUMBER: 68171-52-8
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 25 mg/ml soluble in DMSO or dimethyl formamide; 100μg/ml soluble in a 1:2 solution of ethanol:PBS (pH 7.2) (dilute the ethanol solution with PBS).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.
HANDLING: Keep under inert gas. Protect from light.

Product Description
Endocannabinoid. Does also bind to TRPV1 (Ki=5.60µM).
Product Specific Literature References
Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor: L. Hanus, et al.; J. Med. Chem. 36, 3032 (1993) Abstract
Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens: R.A. Ross, et al.; Br. J. Pharmacol. 132, 631 (2001) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
TRPV1 Agonists and Antagonists / Related Products
 
 
ALX-340-044 Revised 04-Feb-05
Linvanil
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
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ALX-340-044-M005   5 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C26H39NO3
MW: 413.6
PURITY: ≥92%
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Ligand of TRPV1 with low affinity to CB1 receptor (Ki=3.4µM). Also inhibits anandamide uptake (IC50=8.0µM).
Product Specific Literature References
Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors: D. Melck, et al.; BBRC 262, 275 (1999) Abstract
Anandamide uptake by human endothelial cells and its regulation by nitric oxide: M. Maccarrone, et al.; J. Biol. Chem. 275, 13484 (2000) Abstract; Full Text
Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity: L. De Petrocellis, et al.; FEBS Lett. 483, 52 (2000) Abstract
Hypolocomotor effects in rats of capsaicin and two long chain capsaicin homologues: V. Di Marzo, et al.; Eur. J. Pharmacol. 420, 123 (2001) Abstract
The uptake by cells of 2-arachidonoylglycerol, an endogenous agonist of cannabinoid receptors: T. Bisogno, et al.; Eur. J. Biochem. 268, 1982 (2001) Abstract
Further Categories Containing This Product:
Cannabinoid Receptor Agonists & Antagonists / Related Products • Anandamide Uptake Inhibitors
 
 
ALX-340-030 Revised 08-Jul-08
R-1 Methanandamide
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SYNONYMS (R)-(+)-Arachidonyl-1'-hydroxy-2'-propylamide
AM 356
N-(2-Hydroxy-1R-methylethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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ALX-340-030-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C23H39NO2
MW: 361.6
CAS NUMBER: 157182-49-5
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 10mg/ml soluble in DMSO or dimethyl formamide; sparingly soluble in aqueous buffers. To prevent oxidation, the solvent should be purged with an inert gas.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. Keep aqueous solutions on ice and use within 12 hours.
HANDLING: Protect from light and oxygen.
HAZARD: IRRITANT.

Product Description
Amidase resistant cannabinoid receptor (CB) agonist (CB1: Ki=20nM; CB2: Ki=815nM). The most potent of the series of methyl-anandamides. About 4-fold higher binding affinity for cannabinoid receptor CB1 than anandamide (Prod. No. ALX-340-029) in the presence of PMSF. Does also bind to TRPV1 (Ki=4.67µM).
Product Specific Literature References
(R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability: V. Abadji, et al.; J. Med. Chem. 37, 1889 (1994) Abstract
Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand: A.D. Khanolkar, et al.; J. Med. Chem. 39, 4515 (1996) Abstract
Extrapyramidal effects of methanandamide, an analog of anandamide, the endogenous CB1 receptor ligand: J. Romero, et al.; Life Sci. 58, 1249 (1996) Abstract
Substrate specificity and stereoselectivity of rat brain microsomal anandamide amidohydrolase: W. Lang, et al.; J. Med. Chem. 42, 896 (1999) Abstract
Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide: P.M. Zygmunt, et al.; Nature 400, 452 (1999) Abstract
Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens: R.A. Ross, et al.; Br. J. Pharmacol. 132, 631 (2001) Abstract
Up-regulation of cyclooxygenase-2 expression is involved in R(+)-methanandamide-induced apoptotic death of human neuroglioma cells: B. Hinz, et al.; Mol. Pharmacol. 66, 1643 (2004) Abstract; Full Text
R(+)-Methanandamide Elicits a Cyclooxygenase-2-Dependent Mitochondrial Apoptosis Signaling Pathway in Human Neuroglioma Cells: K. Eichele, et al.; Pharm. Res. 23, 90 (2006) Abstract
Antagonism of discriminative stimulus effects of Delta(9)-THC and (R)-methanandamide in rats: T.U. Jarbe, et al.; Psychopharmacology (Berlin) 184, 36 (2006) Abstract
R(+)-methanandamide elicits a cyclooxygenase-2-dependent mitochondrial apoptosis signaling pathway in human neuroglioma cells: K. Eichele, et al.; Pharm. Res. 23, 90 (2006) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Cannabinoid Receptor Agonists & Antagonists / Related Products • TRPV1 Agonists and Antagonists / Related Products
 
 
ALX-550-396 Revised 28-Jun-07
MSK-195
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SYNONYMS N-[2-(3,4-Dimethylbenzyl)-3-(pivalyloxy)propyl]-2-[4-(2-aminoethoxy)-3-methoxyphenyl]acetamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
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ALX-550-396-M001   1 mg 70.00 USD Add To Cart
ALX-550-396-M005   5 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C28H40N2O5
MW: 484.6
CAS NUMBER: 289902-82-5
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, DMSO or other organic solvents; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent analgesic with EC50=0.96µg/kg in the acetic acid-induced writhing test. RTX binding affinity (Ki=603nM), agonism (calcium influx; EC50=240nM).
Product Specific Literature References
Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics: J. Lee, et al.; Bioorg. Med. Chem. 10, 1171 (2002) Abstract
 
 
ALX-550-239 Revised 01-Dec-05
Nonivamide
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SYNONYMS Nonylic vanillylamide
N-[4-Hydroxy-3-methoxy-benzyl]nonanamide
N-Vanillylnonamide
Pelargonic acid vanillylamide
Vanillyl pelargonic amide
Pseudocapsaicin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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ALX-550-239-M025   25 mg 25.00 USD Add To Cart
ALX-550-239-M100   100 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C17H27NO3
MW: 293.4
CAS NUMBER: 2444-46-4
RTECS: RA5955000
SOURCE/HOST: Synthetic
PURITY: ≥96%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: IRRITANT. POTENT NEUROTOXIN.

Product Description
Minor constituent of hot pepper (Capsicum oleoresin).
Product Specific Literature References
The effects of a series of capsaicin analogues on nociception and body temperature in the rat: A.G. Hayes, et al.; Life Sci. 34, 1241 (1984) Abstract
Comparison of nonivamide and capsaicin with regard to their pharmacokinetics and effects on sensory neurons: G. Skofitsch, et al.; Arzneimittel-Forschung 34, 154 (1984) Abstract
Hypotensive and antinociceptive effect of ether-linked and relatively non-pungent analogues of N-nonanoyl vanillylamide: J. Chen, et al.; Eur. J. Med. Chem. 27, 187 (1992)
A possible role of nitric oxide formation in the vasodilatation of rabbit ear artery induced by a topically applied Capsaicin analogue: T. Suzuki, et al.; J. Vet. Med. Sci. 60, 691 (1998) Abstract
The Effect of the Base on the Kinetics of Action of the Capsaicinoid Nonivamide: Evaluation with a Hyperemic Test: M. Stücker, et al.; Skin Pharmacol. Appl. Skin Physiol. 12, 289 (1999) Abstract
Nitrated nonivamide displaying a drawback of proton's role in capsaicin- associated sensory and neuronal activities: Y.C. Yang, et al.; Gen. Pharmacol. 33, 257 (1999) Abstract
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Further Categories Containing This Product:
TRPV1 Agonists and Antagonists / Related Products
 
 
ALX-550-398 Revised 10-Jul-08
N-Oleoyldopamine
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SYNONYMS OLDA
N-[2-(3,4-Dihydroxyphenyl)ethyl]-9Z-octadecenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
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ALX-550-398-M005   5 mg 35.00 USD Add To Cart
Product Specification
FORMULA: C26H43NO3
MW: 417.6
CAS NUMBER: 105955-11-1
CONCENTRATION: 50mg/ml 
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 20mg/ml soluble in DMSO or dimethyl formamide; 0.5mg/ml soluble in a 1:1 solution of ethanol:PBS (pH 7.2) (dilute the ethanol solution with PBS).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.
HANDLING: Protect from light.

Product Description
Endogenous TRPV1 agonist (Ki=36nM, EC50=36nM) with weak affinity for rat CB1 receptor (Ki=1.6µM). Potent inhibitor of 5-lipoxygenase (IC50=7.5nM) and of early and late events in TCR mediated T cell activation. Inhibits NF-κB dependent transcriptional activity without affecting either degradation of the cytoplasmic NF-κB inhibitory protein, IκBα, or DNA binding activity.
Product Specific Literature References
Inhibition of arachidonate 5-lipoxygenase by phenolic compounds: S. Iwakami, et al.; Chem. Pharm. Bull. 34, 3960 (1986) Abstract
Inhibition of in vitro prostaglandin and leukotriene biosyntheses by cinnamoyl-beta-phenethylamine and N-acyldopamine derivatives: C.F. Tseng, et al.; Chem. Pharm. Bull. 40, 396 (1992) Abstract
N-oleoyldopamine, a novel endogenous capsaicin-like lipid that produces hyperalgesia: C.J. Chu, et al.; J. Biol. Chem. 278, 13633 (2003) Abstract
Direct evidence for activation and desensitization of the capsaicin receptor by N-oleoyldopamine on TRPV1-transfected cell, line in gene deleted mice and in the rat: J. Szolcsanyi, et al.; Neurosci. Lett. 361, 155 (2004) Abstract
Immunosuppressive activity of endovanilloids: N-arachidonoyl-dopamine inhibits activation of the NF-kappa B, NFAT, and activator protein 1 signaling pathways: R. Sancho, et al.; J. Immunol. 172, 2341 (2004) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Endovanilloids • Lipoxygenases / Related Products • NF-kB Pathway Inhibitors
 
 
ALX-300-150 Revised 11-Oct-07
Oleoylethanolamide
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SYNONYMS N-(2-Hydroxyethyl)-9Z-octadecenamide
OEA
PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
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ALX-300-150-M005   5 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C20H39NO2
MW: 325.5
CAS NUMBER: 111-58-0
PURITY: ≥99%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Activates TRPV1. Does not activate cannabinoid receptors (CB) but is a PPARα agonist (EC50=120nM) in vitro and in vivo; induces satiety through activation of PPARα. Inhibits ceramidase.
Product Specific Literature References
Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor: L. Hanus, et al.; J. Med. Chem. 36, 3032 (1993) Abstract
Differential regulation of sphingomyelinase and ceramidase activities by growth factors and cytokines. Implications for cellular proliferation and differentiation: E. Coroneos, et al.; J. Biol. Chem. 270, 23305 (1995) Abstract
Cannabinomimetic behavioral effects of and adenylate cyclase inhibition by two new endogenous anandamides: J. Barg, et al.; Eur. J. Pharmacol. 287, 145 (1995) Abstract
A peripheral mechanism for CB1 cannabinoid receptor-dependent modulation of feeding: R. Gomez, et al.; J. Neurosci. 22, 9612 (2002) Abstract
Activation of TRPV1 by the satiety factor oleoylethanolamide: G.P. Ahern; J. Biol. Chem. 278, 30429 (2003) Abstract
Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-alpha: J. Fu, et al.; Nature 425, 90 (2003) Abstract
Oleoylethanolamide stimulates lipolysis by activating the nuclear receptor PPAR-alpha: M. Guzman, et al.; J. Biol. Chem. 279, 27849 (2004)
Further Categories Containing This Product:
Anandamide & Anandamide Analogs • PPAR Agonists
 
 
ALX-340-041 Revised 11-Dec-07
Olvanil
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SYNONYMS NE-19550
N-Vanillyloleoylamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-041-M005   5 mg 30.00 USD Add To Cart
ALX-340-041-M010   10 mg 48.00 USD Add To Cart
Product Specification
FORMULA: C26H43NO3
MW: 417.6
CAS NUMBER: 58493-49-5
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, chloroform, dimethyl formamide or DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
"Hybrid" activator of CB1 receptor (CB1: Ki=1.6µM; CB2: Ki=15µM) and TRPV1 (Ki=0.4µM; EC50=33nM (human); EC50=6.71nM (rat)). Also inhibits anandamide uptake (IC50=9µM, Ki=14.1µM) and fatty acid amide hydrolase (FAAH) (IC50=20µM).
Product Specific Literature References
NE-19550: a novel, orally active anti-inflammatory analgesic: L. Brand, et al.; Drugs Exp. Clin. Res. 13, 259 (1987) Abstract
The antinociceptive effect and pharmacokinetics of olvanil following oral and subcutaneous dosing in the mouse: W.K. Sietsema, et al.; Life Sci. 43, 1385 (1988) Abstract
Olvanil: more potent than capsaicin at stimulating the efferent function of sensory nerves: S.R. Hughes, et al.; Eur. J. Pharmacol. 219, 481 (1992) Abstract
Interactions between synthetic vanilloids and the endogenous cannabinoid system: V. Di Marzo, et al.; FEBS Lett. 436, 449 (1998) Abstract
Anandamide transport inhibition by the vanilloid agonist olvanil: M. Beltramo & D. Piomelli; Eur. J. Pharmacol. 364, 75 (1999) Abstract
Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors: D. Melck, et al.; BBRC 262, 275 (1999) Abstract
Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide: P.M. Zygmunt, et al.; Nature 400, 452 (1999) Abstract
Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity: L. De Petrocellis, et al.; FEBS Lett. 483, 52 (2000) Abstract
Characterization using FLIPR of rat vanilloid receptor (rVR1) pharmacology: J.C. Jerman, et al.; Br. J. Pharmacol. 130, 916 (2000) Abstract
Evidence against the presence of an anandamide transporter: S.T. Glaser, et al.; PNAS 100, 4269 (2003) Abstract
Identification of species-specific determinants of the action of the antagonist capsazepine and the agonist PPAHV on TRPV1: E. Phillips, et al.; J. Biol. Chem. 279, 17165 (2004) Abstract
Effects of the vanilloid agonist olvanil and antagonist capsazepine on rat behaviors: J.W. Kasckow, et al.; Prog. Neuropsychopharmacol. Biol. Psychiatry 28, 291 (2004) Abstract
Further Categories Containing This Product:
Anandamide Uptake Inhibitors • Cannabinoid Receptor Agonists & Antagonists / Related Products • Fatty Acid Amide Hydrolase [FAAH] / Related Products
 
 
ALX-550-355 Revised 30-Jun-08
PPAHV