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Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-270-239 Revised 19-Jun-08
AM 251
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SYNONYMS N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-270-239-M001   1 mg 29.00 USD Add To Cart
ALX-270-239-M005   5 mg 131.00 USD Add To Cart
Product Specification
FORMULA: C22H21Cl2IN4O
MW: 555.2
CAS NUMBER: 183232-66-8
PURITY: ≥98%
APPEARANCE: White to light pink solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C

Product Description
Structurally related to the cannabinoid receptor (CB) antagonist SR 141716A. Binds with high affinity to cannabinoid receptor CB1 (Ki=7.49nM; 306-fold selective over CB2 receptors).
Product Specific Literature References
Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors: S.J. Gatley, et al.; Life Sci. 61, PL 191 (1997) Abstract
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists: R. Lan, et al.; J. Med. Chem. 42, 769 (1999) Abstract
Inhibition of voltage-sensitive sodium channels by the cannabinoid 1 receptor antagonist AM 251 in mammalian brain: C. Liao, et al.; Basic Clin. Pharmacol. Toxicol. 94, 73 (2004) Abstract
Cannabinoid (CB)1 receptor antagonist, AM 251, causes a sustained reduction of daily food intake in the rat: A.P. Chambers, et al.; Physiol. Behav. 82, 863 (2004) Abstract
The cannabinoid CB1 antagonist AM 251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats: P.J. McLaughlin, et al.; Psychopharmacology (Berlin) 180, 286 (2005) Abstract
The cannabinoid 1 receptor antagonist, AM251, prolongs the survival of rats with severe acute pancreatitis: K. Matsuda, et al.; Tohoku J. Exp. Med. 207, 99 (2005) Abstract; Full Text
Anxiogenic profile of AM-251, a selective cannabinoid CB1 receptor antagonist, in plus-maze-naive and plus-maze-experienced mice: R.J. Rodgers, et al.; Behav. Pharmacol. 16, 405 (2005) Abstract
AM 251 produces sustained reductions in food intake and body weight that are resistant to tolerance and conditioned taste aversion: A.P. Chambers, et al.; Br. J. Pharmacol. 147, 109 (2006) Abstract; Full Text
 
 
ALX-270-240 Revised 05-May-08
AM 281
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SYNONYMS 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-270-240-M001   1 mg 25.00 USD Add To Cart
ALX-270-240-M005   5 mg 70.00 USD Add To Cart
ALX-270-240-M025   25 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C21H19Cl2IN4O2
MW: 557.2
CAS NUMBER: 202463-68-1
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in methanol (1mg/ml) or DMSO (2mg/ml at RT, 50mg/ml in hot DMSO, after cooling this solution is stable over several days.)
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Identity determined by 1H-NMR.

Product Description
Analog of the cannabinoid receptor (CB) antagonist SR 141716A. Potent CB1 receptor antagonist/inverse agonist (Ki=14nM).
Product Specific Literature References
Effect of the cannabinoid receptor SPECT agent, AM 281, on hippocampal acetylcholine release from rat brain slices: A.N. Gifford, et al.; Neurosci. Lett. 238, 84 (1997) Abstract
Imaging the brain marijuana receptor: development of a radioligand that binds to cannabinoid CB1 receptors in vivo: S.J. Gatley, et al.; J. Neurochem. 70, 417 (1998) Abstract
Large receptor reserve for cannabinoid actions in the central nervous system: A. N. Gifford, et al.; J. Pharmacol. Exp. Ther. 288, 478 (1999) Abstract
Effects of the cannabinoid antagonists AM281 and AM630 on deprivation-induced intake in Lewis rats: N.A. Werner, et al.; Brain Res. 967, 290 (2003) Abstract
Effects of AM281, a cannabinoid antagonist, on systemic haemodynamics, internal carotid artery blood flow and mortality in septic shock in rats: Y. Kadoi, et al.; Br. J. Anaesth. 94, 563 (2005) Abstract
Cannabinoid antagonist AM 281 reduces mortality rate and neurologic dysfunction after cecal ligation and puncture in rats: Y. Kadoi, et al.; Crit. Care Med. 33, 2629 (2005) Abstract
 
 
ALX-270-241 Revised 03-Mar-05
AM 630
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SYNONYMS (6-Iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl)(4-methoxyphenyl)methanone
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-270-241-M001   1 mg 20.00 USD Add To Cart
ALX-270-241-M005   5 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C23H25IN2O3
MW: 504.4
CAS NUMBER: 164178-33-0
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and oxygen.

Product Description
Competitive CB1 receptor antagonist in guinea-pig brain. Shows also agonist properties. CB2 antagonist/inverse agonist (Ki=31.2nM; 165-fold selective over CB1 receptors).
Product Specific Literature References
AM630, a competitive cannabinoid receptor antagonist: R. Pertwee, et al.; Life Sci. 56, 1949 (1995) Abstract
AM630 is a competitive cannabinoid receptor antagonist in the guinea pig brain: K. Hosohata, et al.; Life Sci. 61, PL115 (1997) Abstract
AM630 antagonism of cannabinoid-stimulated [35S]GTP gamma S binding in the mouse brain: Y. Hosohata, et al.; Eur. J. Pharmacol. 321, R1 (1997) Abstract
AM630 is an inverse agonist at the human cannabinoid CB1 receptor: R.S. Landsman, et al.; Life Sci. 62, PL109 (1998) Abstract
Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630: R.A. Ross, et al.; Br. J. Pharmacol. 126, 665 (1999) Abstract
Effects of the cannabinoid antagonists AM281 and AM630 on deprivation-induced intake in Lewis rats: N.A. Werner, et al.; Brain Res. 967, 290 (2003) Abstract
 
 
ALX-550-383 Revised 11-Apr-07
AM 1241
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SYNONYMS (2-Iodo-5-nitrophenyl)-(1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl)methanone
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-550-383-M001   1 mg 40.00 USD Add To Cart
ALX-550-383-M005   5 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C22H22N3O3I
MW: 503.3
PURITY: ≥97% (TLC)
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, 100% ethanol or methanol; insoluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Unstable in 1M NaOH; slightly unstable in 1M HCl.
HANDLING: Packaged under inert gas. Protect from light.

Product Description
Potent and selective CB2 receptor agonist (Ki=3.4nM (mouse), Ki=280nM (rat) also in vivo.
Product Specific Literature References
CB2 cannabinoid receptor-mediated peripheral antinociception: T.P. Malan, Jr., et al.; Pain 93, 239 (2001) Abstract
Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not present in the CNS: M.M. Ibrahim, et al.; PNAS 100, 10529 (2003) Abstract; Full Text
Selective activation of cannabinoid CB(2) receptors suppresses spinal fos protein expression and pain behavior in a rat model of inflammation: A.G. Nackley, et al.; Neuroscience 119, 747 (2003) Abstract
Inhibition of inflammatory hyperalgesia by activation of peripheral CB2 cannabinoid receptors: A. Quartilho, et al.; Anesthesiology 99, 955 (2003) Abstract
Selective activation of cannabinoid CB2 receptors suppresses hyperalgesia evoked by intradermal capsaicin: A.G. Hohmann, et al.; J. Pharmacol. Exp. Ther. 308, 446 (2004) Abstract
In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor?: B.B. Yao, et al.; Br. J. Pharmacol. 149, 145 (2006) Abstract
 
 
ALX-340-053 Revised 04-Aug-08
Arachidonoyl 2’-chloroethylamide
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SYNONYMS ACEA
N-(2-Chloroethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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ALX-340-053-M005   5 mg 46.00 USD Add To Cart
Product Specification
FORMULA: C22H36NOCl
MW: 366.0
CAS NUMBER: 220556-69-4
CONCENTRATION: 10mg/ml
PURITY: ≥96%
FORMULATION: Liquid. Solution in methyl acetate.
SOLUBILITY: 20mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; 250μg/ml soluble in a 1:3 solution of ethanol:PBS (pH 7.2) (dilute the ethanol solution with PBS).
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -80°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -80°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Non-pungent, potent and highly selective CB1 receptor agonist (Ki=1.4nM). Displays >1'400-fold selectivity over CB2 receptors (Ki=3.1µM). Active in vivo.
Product Specific Literature References
Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1): C.J. Hillard, et al.; J. Pharmacol. Exp. Ther. 289, 1427 (1999) Abstract
Arachidonylcyclopropylamide increases microglial cell migration through cannabinoid CB2 and abnormal-cannabidiol-sensitive receptors: A. Franklin, et al.; Eur. J. Pharmacol. 474, 195 (2003) Abstract
Modulation of trigeminal sensory neuron activity by the dual cannabinoid-vanilloid agonists anandamide, N-arachidonoyl-dopamine and arachidonyl-2-chloroethylamide: T.J. Price, et al.; Br. J. Pharmacol. 141, 1118 (2004) Abstract
The cannabinomimetic arachidonyl-2-chloroethylamide (ACEA) acts on capsaicin-sensitive TRPV1 receptors but not cannabinoid receptors in rat joints: C.L. Baker and J.J. McDougall; Br. J. Pharmacol. 142, 1361 (2004) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Cannabinoid Receptor Agonists & Antagonists / Related Products
 
 
ALX-340-054 Revised 09-Jul-08
Arachidonoyl cyclopropylamide
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SYNONYMS ACPA
N-Cyclopropyl-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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ALX-340-054-M005   5 mg 46.00 USD Add To Cart
Product Specification
FORMULA: C23H37NO
MW: 343.6
CAS NUMBER: 229021-64-1
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 10mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; 1mg/ml soluble in a 1:1 solution of in 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 CB1 agonist (Ki=2.2nM). Displays 325-fold selectivity over CB2 receptors (Ki=0.7µM). Active in vivo.
Product Specific Literature References
Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1): C.J. Hillard, et al.; J. Pharmacol. Exp. Ther. 289, 1427 (1999) Abstract
Arachidonylcyclopropylamide increases microglial cell migration through cannabinoid CB2 and abnormal-cannabidiol-sensitive receptors: A. Franklin, et al.; Eur. J. Pharmacol. 474, 195 (2003) Abstract
The interaction of cannabinoids and opioids on pentylenetetrazole-induced seizure threshold in mice: H. Shafaroodi, et al.; Neuropharmacology 47, 390 (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:
Cannabinoid Receptor Agonists & Antagonists / Related Products
 
 
ALX-340-061 Revised 10-Jul-08
Arachidonoyl 2'-fluoroethylamide
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SYNONYMS N-(2-Fluoroethyl)-5Z,8Z,11Z,14Z-eicosatetraenamide
2'-Fluoro AEA
2'-Fluoro anandamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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ALX-340-061-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C22H36NOF
MW: 349.5
CAS NUMBER: 166100-37-4
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 7mg/ml soluble in DMSO or dimethyl formamide; 8mg/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.

Product Description
CB1 receptor agonist (CB1: Ki=26.7nM; CB2: Ki=908nM).
Product Specific Literature References
Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability: S. Lin, et al.; J. Med. Chem. 41, 5353 (1998) 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
 
 
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
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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
 
 
ALX-550-524 Revised 19-Jul-07
1,3-bis(4-Bromophenyl)-5-phenyl-2,4-imidazolidinedione
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SYNONYMS Compound 25
CB1 Cannabinoid Receptor Inverse Agonist
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-550-524-M005   5 mg 25.00 USD Add To Cart
Product Specification
FORMULA: C21H14Br2N2O2
MW: 486.2
CAS NUMBER: 878533-35-8
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; sparingly soluble in aqueous buffers.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 2 years after receipt when stored at -20°C.

Product Description
Potent and selective inverse agonist of CB1 receptor (Ki=243nM and EC50=195nM).
Product Specific Literature References
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists: G.G. Muccioli, et al.; J. Med. Chem. 49, 872 (2006) Abstract
 
 
ALX-430-152 Revised 03-Apr-08
Cannabidiol
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SYNONYMS CBD
2-[(1R,6R)-3-Methyl-6-(1-methylethenyl)-2-cyclohexen-1-yl]-5-pentyl-1,3-benzenediol
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-430-152-M001   1 mg