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TRPV1 Agonists and Antagonists / Related Products
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ALX-300-148 Revised 11-Jul-08
Docosatetraenylethanolamide
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SYNONYMS N-(2-Hydroxyethyl)-7Z,10Z,13Z,16Z-docosatetraenamide
DEA
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Endocannabinoids
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ALX-300-148-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C24H41NO2
MW: 375.6
CAS NUMBER: 150314-35-5
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 10mg/ml soluble in DMSO or dimethyl formamide; 8mg/ml soluble in 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: Protect from light.

Product Description
Endocannabinoid. Also inhibits adenylate cyclase (IC50=117nM). Does also bind to TRPV1 (Ki=5.63µM).
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
Anandamide, an endogenous cannabimimetic eicosanoid, binds to the cloned human cannabinoid receptor and stimulates receptor-mediated signal transduction: C.C. Felder, et al.; PNAS 90, 7656 (1993) 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
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
Astrocytes in culture produce anandamide and other acylethanolamides: L. Walter, et al.; J. Biol. Chem. 277, 20869 (2002) 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:
Adenylyl Cyclase Inhibitors • TRPV1 Agonists and Antagonists / Related Products • Fatty Acids
 
 
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-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-340-030 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-340-032 Revised 04-Jul-08
AM 404
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SYNONYMS N-(4-Hydroxyphenyl)-5Z,8Z,11Z-eicosatetraenamide
N-(4-Hydroxyphenyl)arachidonoylamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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ALX-340-032-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C26H37NO2
MW: 395.6
CAS NUMBER: 198022-70-7
PURITY: ≥98%
APPEARANCE: Waxy solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol (>25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for up to one year after receipt when stored at -20°C. Solutions are stable for up to 3 months when stored at -20°C under an inert atmosphere of nitrogen or argon.
HANDLING: Protect from air.

Product Description
Analog of anandamide (Prod. No. ALX-340-029). Potentiates the activity of endogenous anandamide by blocking its re-uptake into presynaptic membranes. Activates TRPV1 (EC50=0.04µM) at concentrations lower than those required to inhibit anandamide transport into the cell (neuronal (C6 glioma cells): IC50=10µM; non-neuronal (rat RBL-2H3 cells): IC50=11µM). Low affinity to FAAH (IC50=5.9µM), to CB1 receptor (IC50=1.76µM) and to CB2 receptor (IC50>1µM).
Product Specific Literature References
Potentiation of anandamide hypotension by the transport inhibitor, AM404: A. Calignano, et al.; Eur. J. Pharmacol. 337, R1 (1997) Abstract
Functional role of high-affinity anandamide transport, as revealed by selective inhibition: M. Beltramo, et al.; Science 277, 1094 (1997) Abstract
Structural determinants for recognition and translocation by the anandamide transporter: D. Piomelli, et al.; PNAS 96, 5802 (1999) Abstract
The anandamide transport inhibitor AM404 activates vanilloid receptors: P.M. Zygmunt, et al.; Eur. J. Pharmacol. 396, 39 (2000) 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
Experimental parkinsonism alters anandamide precursor synthesis, and functional deficits are improved by AM404: a modulator of endocannabinoid function: E. Fernandez-Espejo, et al.; Neuropsychopharmacology 29, 1134 (2004) Abstract
Anandamide transport inhibitor AM404 and structurally related compounds inhibit synaptic transmission between rat hippocampal neurons in culture independent of cannabinoid CB1 receptors: B.G. Kelley and S.A. Thayer; Eur. J. Pharmacol. 496, 33 (2004) Abstract
AM404, an inhibitor of anandamide uptake, prevents pain behaviour and modulates cytokine and apoptotic pathways in a rat model of neuropathic pain: B. Costa, et al.; Br. J. Pharmacol. 148, 1022 (2006) Abstract
Modulation of neuropathic and inflammatory pain by the endocannabinoid transport inhibitor AM404 [N-(4-hydroxyphenyl)-eicosa-5,8,11,14-tetraenamide]: G. La Rana, et al.; J. Pharmacol. Exp. Ther. 317, 1365 (2006) Abstract
Further Categories Containing This Product:
NOS Inhibitors (NOS Induction & Enzyme Activity) • Anandamide Uptake Inhibitors • TRPV1 Agonists and Antagonists / Related Products
 
 
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
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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-340-042 Revised 07-Jan-06
Arvanil
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SYNONYMS N-[(4-Hydroxy-3-methoxyphenyl)methyl]-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-042-M005   5 mg 25.00 USD Add To Cart
Product Specification
FORMULA: C28H41NO3
MW: 439.6
CAS NUMBER: 128007-31-8
PURITY: ≥98%
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry.

Product Description
"Hybrid" activator of CB1 receptor (CB1: Ki=0.5µM; CB2: Ki=>15µM) and TRPV1 (Ki=0.3µM). Also inhibits anandamide uptake (IC50=3.6µM) and fatty acid amide hydrolase (FAAH) (IC50=3µM). Analgesic, vasodilatory and anti-inflammatory in vivo. Apoptosis inducer.
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
Neurobehavioral activity in mice of N-vanillyl-arachidonyl-amide: V. Di Marzo, et al.; Eur. J. Pharmacol. 406, 363 (2000) Abstract
A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid: V. Di Marzo, et al.; J. Pharmacol. Exp. Ther. 300, 984 (2002) Abstract
The CB1/VR1 agonist arvanil induces apoptosis through an FADD/caspase-8-dependent pathway: R. Sancho, et al.; Br. J. Pharmacol. 140, 1035 (2003) Abstract
Evidence against the presence of an anandamide transporter: S.T. Glaser, et al.; PNAS 100, 4269 (2003) Abstract
Arvanil, a hybrid endocannabinoid and vanilloid compound, behaves as an antihyperkinetic agent in a rat model of Huntington's disease: E. de Lago, et al.; Brain Res. 1050, 210 (2005) Abstract
Arvanil inhibits T lymphocyte activation and ameliorates autoimmune encephalomyelitis: A.M. Malfitano, et al.; J. Neuroimmunol. 171, 110 (2006) Abstract
Further Categories Containing This Product:
Anandamide Uptake Inhibitors • Apoptosis Inducers & Inhibitors Other Products • TRPV1 Agonists and Antagonists / Related Products • Analgesic / Anti-nociceptive Agents / Related Products • Anti-inflammatory Agents Other Products • Fatty Acid Amide Hydrolase [FAAH] / 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-340-056 Revised 09-Jul-08
UCM707
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SYNONYMS N-(3-Furanylmethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-056-M005   5 mg 101.00 USD Add To Cart
Product Specification
FORMULA: C25H37NO2
MW: 383.6
CAS NUMBER: 390824-20-1
PURITY: ≥98%
FORMULATION: Liquid. Solution in methyl acetate.
SOLUBILITY: 20mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; 250μg/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.

Product Description
Potent and selective anandamide uptake inhibitor (neuronal (C6 glioma cells): IC50=25µM; non-neuronal (rat RBL-2H3 cells): IC50=41µM) with low affinity to CB1 receptor (CB1: Ki=4.8µM; CB2: Ki=0.067µM). Inhibits TRPV1 (Ki>5µM) and FAAH (IC50>100µM). Potentiates hypokinetic and antinociceptive effects of anandamide in vivo.
Product Specific Literature References
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors: M.L. Lopez-Rodriguez, et al.; J. Med. Chem. 44, 4505 (2001) Abstract
UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinocicep