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Neurobiology
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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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-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:
Anandamide Uptake Inhibitors • NOS Inhibitors (NOS Induction & Enzyme Activity) • TRPV1 Agonists and Antagonists/Related Products
 
 
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-550-212 Revised 17-Jan-05
Amiloride . hydrochloride
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SYNONYMS 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-212-G001   1 g 23.00 USD Add To Cart
Product Specification
FORMULA: C6H8ClN7O . HCl
MW: 229.6 . 36.5
CAS NUMBER: 2016-88-8
MERCK INDEX: 14: 406
PURITY: ≥98%
APPEARANCE: Light yellow solid.
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: TOXIC.

Product Description
Epithelial Na+ channel inhibitor [1]. Selective T-type Ca2+ channel blocker [2].
Product Specific Literature References
[1] Amiloride and its analogs as tools in the study of ion transport: T.R. Kleyman and E.J. Kragoe Jr.; J. Membr. Biol. 105, 1 (1988) Abstract
[2] Amiloride selectively blocks the low threshold (T) calcium channel: C.-M. Tang, et al.; Science 240, 213 (1988) Abstract
Further Categories Containing This Product:
Ca2+ Channels (T-type) • Imidazoline Binding Site Ligands
 
 
ALX-550-261 Revised 16-Apr-05
Amiloride, 5-(N,N-Dimethyl)-, . hydrochloride
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SYNONYMS 5-(N,N-Dimethyl)amiloride . HCl
DMA . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-261-M005   5 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C8H12ClN7O . HCl
MW: 257.7 . 36.5
CAS NUMBER: 1214-79-5 (free base)
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in methanol (10mg/ml) or water (6mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Na+/H+ antiporter inhibitor (IC50=6.9 µM) with increased selectivity and potency relative to amiloride (Prod. No. ALX-550-212).
Product Specific Literature References
Involvement of sodium in the protective effect of 5-(N,N-dimethyl)- amiloride on ischemia-reperfusion injury in isolated rat ventricular wall: H. Meng & G.N. Pierce; J. Pharmacol. Exp. Ther. 256, 1094 (1991) Abstract
Amiloride and its analogs as tools in the study of ion transport: T.R. Kleyman & E.J. Cragoe Jr.; J. Membr. Biol. 105, 1 (1988) Abstract
Effect of 5-(N,N-Dimethyl)-amiloride, a specific inhibitor of Na(+)/H(+) exchanger, on the palmitoyl-L-carnitine-induced mechanical and metabolic derangements in the isolated perfused rat heart: J. Arakawa & A. Hara; Pharmacology 59, 239 (1999) Abstract
Hypericin-induced phototoxicity of human leukemic cell line HL-60 is potentiated by omeprazole, an inhibitor of H+K+-ATPase and 5'-(N,N-dimethyl)-amiloride, an inhibitor of Na+/H+ exchanger: L. Mirossay, et al.; Physiol. Res. 48, 135 (1999) Abstract
Further Categories Containing This Product:
Imidazoline Binding Site Ligands • Ca2+ Channels (T-type)
 
 
ALX-550-266 Revised 12-Feb-08
Amiloride, 5-(N-Ethyl-N-isopropyl)-
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SYNONYMS 5-(N-Ethyl-N-isopropyl)amiloride
EIPA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-266-M005   5 mg 38.00 USD Add To Cart
Product Specification
FORMULA: C11H18ClN7O
MW: 299.8
CAS NUMBER: 1154-25-2
PURITY: ≥99%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in methanol, DMSO or dilute aqueous acid; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Selective inhibitor of the Na+/H+ antiporter.
Product Specific Literature References
Influence of atrial natriuretic factor on 5-(N-ethyl-N- isopropyl)amiloride-sensitive 22Na+ uptake in rabbit aorta: S. Gupta, et al.; J. Pharmacol. Exp. Ther. 248, 991 (1989) Abstract
Regulation of intracellular pH in crypt cells from rabbit distal colon: S.L. Abrahamse, et al.; Am. J. Physiol. 267, G409 (1994) Abstract
Apical membrane Na+/H+ exchange in rat medullary thick ascending limb. pH-dependence and inhibition by hyperosmolality: B.A. Watts III & D.W. Good; J. Biol. Chem. 269, 20250 (1994) Abstract; Full Text
Further Categories Containing This Product:
Imidazoline Binding Site Ligands • Ca2+ Channels (T-type)
 
 
ALX-550-257 Revised 10-Feb-05
Amiloride, 5-(N-Methyl-N-isobutyl)-
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SYNONYMS 5-(N-Methyl-N-isobutyl)amiloride
MIA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
Ordering Information
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ALX-550-257-M005   5 mg 25.00 USD Add To Cart
Product Specification
FORMULA: C11H18ClN7O
MW: 299.8
CAS NUMBER: 96861-65-3
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in dilute aqueous acid or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Potent inhibitor of the Na+/H+ antiporter. Possible antitumor agent.
Product Specific Literature References
Interactions of chloride and amiloride with the renal Na+/H/ antiporter: D.G. Warnock, et al.; J. Biol. Chem. 263, 7216 (1988) Abstract; Full Text
Methyl isobutyl amiloride: a new probe to assess the number of Na-H antiporters: Z. Talor, et al.; Life Sci. 45, 517 (1989) Abstract
Therapeutic potential of analogues of amiloride: inhibition of the regulation of intracellular pH as a possible mechanism of tumour selective therapy: R.P. Maidorn, et al.; Br. J. Cancer. 67, 297 (1993) Abstract
Study of fibroblast spreading: pH dependence, involvement of the Na+/H(+)-antiporter and PKC: I.Y. Novikova, et al.; Biochim. Biophys. Acta 1178, 267 (1993) Abstract
Methyl isobutyl amiloride alters regional brain reperfusion after resuscitation from cardiac arrest in rats: K.L. Lauro, et al.; Brain Res. 831, 64 (1999) Abstract
Role of Na(+)/H(+) exchanger during ischemia and preconditioning in the isolated rat heart: X.H. Xiao & D.G. Allen; Circ. Res. 85, 723 (1999) Abstract
Further Categories Containing This Product:
Imidazoline Binding Site Ligands • Ca2+ Channels (T-type) • Antitumor Reagents Other Products
 
 
ALX-106-025 Revised 07-May-03
γ-Aminobutyric acid