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G-Protein Coupled Receptor Signalling
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ALX-550-349 Revised 29-Jan-05
PCCG-13
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SYNONYMS (2R,1S,2R,3S)-2-(2-Carboxy-3-phenylcyclopropyl)glycine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-349-M001   1 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C12H13NO4
MW: 235.2
PURITY: ≥90%
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO and 3N HCl; poorly soluble in water and pyridine; insoluble in alcohol. DO NOT DISSOLVE IN BASIC SOLUTION!
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
A potent, selective and competitive antagonist of PLD-coupled mGluRs.
Product Specific Literature References
Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2'-carboxy-3'-phenylcyclopropyl)glycine. Focus on (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptor: R. Pellicciari, et al.; J. Med. Chem. 39, 2259 (1996) Abstract
Pharmacological characterization of metabotropic glutamate receptors coupled to phospholipase D in the rat hippocampus: D.E. Pellegrini-Giampietro, et al.; Br. J. Pharmacol. 118, 1035 (1996) Abstract
(2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties: R. Pellicciari, et al.; J. Med. Chem. 42, 2716 (1999) Abstract
Antagonist pharmacology of metabotropic glutamate receptors coupled to phospholipase D activation in adult rat hippocampus: focus on (2R,1'S,2'R,3'S)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine versus 3, 5-dihydroxyphenylglycine: S. Albani-Torregrossa, et al.; Mol. Pharmacol. 55, 699 (1999) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999) Abstract
 
 
ALX-550-351 Revised 04-Mar-05
(S)-MPPG (cyclic)
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SYNONYMS (S)-1-Amino-5-phosphonoindane-1-carboxylic acid
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-351-M001   1 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C10H12NO5P
MW: 257.2
PURITY: ≥98%
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Selective antagonist of group II mGluRs.
Product Specific Literature References
Synthesis and biological activity of cyclic analogues of MPPG and MCPG as metabotropic glutamate receptor antagonists: D. Ma, et al.; Bioorg. Med. Chem. Lett. 7, 1195 (1997)
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999) Abstract
 
 
ALX-550-359 Revised 12-May-03
1-Benzyl-APDC . hydrochloride
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SYNONYMS 1-Benzyl-(2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-359-M001   1 mg 30.00 USD Add To Cart
ALX-550-359-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C13H16N2O4 . HCl
MW: 264.3 . 36.5
PURITY: ≥97%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
mGlu6 receptor selective ligand.
Product Specific Literature References
Synthesis, molecular modelling and biology of the 1-benzyl derivative of APDC - an apparent mGluR6 selective ligand: W. Tückmantel, et al.; Bioorg. Med. Chem. Lett. 7, 601 (1997)
Synthesis and metabotropic glutamate receptor antagonist activity of N1- substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid: M.J. Valli, et al.; Bioorg. Med. Chem. Lett. 8, 1985 (1998) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999), (Review) Abstract
 
 
ALX-550-360 Revised 19-Aug-02
α-Benzylquisqualic acid
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-360-M001   1 mg 30.00 USD Add To Cart
ALX-550-360-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C12H13N3O5
MW: 279.3
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective antagonist of group II mGluRs.
Product Specific Literature References
alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists: A.P. Kozikowski, et al.; Bioorg. Med. Chem. Lett. 8, 447 (1998) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp; Neuropharmacology 38, 1431 (1999), (Review) Abstract
Further Categories Containing This Product:
AMPA Receptors / Related Products
 
 
ALX-550-367 Revised 06-Mar-03
SIB-1893
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SYNONYMS (E)-2-Methyl-6-(2-phenylethyl)-pyridine
(E)-2-Methyl-6-styryl-pyridine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-367-M005   5 mg 75.00 USD Add To Cart
ALX-550-367-M025   25 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C14H13N
MW: 195.3
CAS NUMBER: 6266-99-5
PURITY: ≥96%
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Selective, noncompetitive antagonist for the mGlu5 receptor. Crosses the blood-brain barrier.
Product Specific Literature References
SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5: M.A. Varney, et al.; J. Pharmacol. Exp. Ther. 290, 170 (1999) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999) Abstract
 
 
ALX-550-368 Revised 23-May-06
MPEP . hydrochloride
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SYNONYMS 6-Methyl-2-(phenylethynyl)-pyridine . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-368-M005   5 mg 45.00 USD Add To Cart
ALX-550-368-M025   25 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C14H11N . HCl
MW: 193.3 . 36.5
CAS NUMBER: 96206-92-7
PURITY: ≥99%
APPEARANCE: Off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent and selective antagonist for mGluR5 receptor. Systemically active in vivo.
Product Specific Literature References
2-Methyl-6-(Phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active MGlu5 receptor antagonist: F. Gasparini, et al.; Neuropharmacology 38, 1493 (1999) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999) Abstract
Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in the thalamus: T.E. Salt, et al.; Br. J. Pharmacol. 127, 1057 (1999) Abstract
Selective blockade of metabotropic glutamate receptor subtype 5 is neuroprotective: V. Bruno, et al.; Neuropharmacology 39, 2223 (2000) Abstract
Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893): A.G. Chapman, et al.; Neuropharmacology 39, 1567 (2000) Abstract
Methylphenylethynylpyridine (MPEP) Novartis: F. Micheli; Curr. Opin. Investig. Drugs 1, 355 (2000) Abstract
Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist: E. Tatarczynska, et al.; Br. J. Pharmacol. 132, 1423 (2001) Abstract; Full Text
Glutamate release inhibiting properties of the novel mGlu(5) receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP): complementary in vitro and in vivo evidence: L.S. Thomas, et al.; Neuropharmacology 41, 523 (2001) Abstract
Evidence that the metabotropic glutamate receptor 5 antagonist MPEP may act as an inhibitor of the norepinephrine transporter in vitro and in vivo: C.A. Heidbreder, et al.; Synapse 50, 269 (2003) Abstract
In the amygdala anxiolytic action of mGlu5 receptors antagonist MPEP involves neuropeptide Y but not GABAA signaling: J.M. Wieronska, et al.; Neuropsychopharmacology 29, 514 (2004) Abstract; Full Text
Chronic treatment with the mGlu5R antagonist MPEP reduces the functional effects of the mGlu5R agonist CHPG in the striatum of 6-hydroxydopamine-lesioned rats: possible relevance to the effects of mGlu5R blockade in Parkinson’s disease: M.R. Domenici, et al.; J. Neurosci. Res. 80, 646 (2005) Abstract
Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats: M. Pietraszek, et al.; Eur. J. Pharmacol. 514, 25 (2005) Abstract
Further Categories Containing This Product:
Anxiolytic Agents / Related Products
 
 
ALX-550-377 Revised 29-Jan-05
(RS)-PPG
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SYNONYMS (RS)-Phosphonophenylglycine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-377-M005   5 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C8H10NO5P
MW: 231.1
CAS NUMBER: 120667-15-4
PURITY: ≥95%
SOLUBILITY: Soluble in diluted NaOH.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent and selective group III mGluR agonist, with a subtype specificity towards the mGlu3 receptor.
Product Specific Literature References
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists [published erratum appears in J. Med. Chem. 32, 2583 (1989)]: C.F. Bigge, et al.; J. Med. Chem. 32, 1580 (1989) Abstract
Neuroprotection in vitro and in vivo by (R,S)-PPG, a potent and selective group III metabotropic glutamate receptor antagonist: P.J. Flor; Soc. Neurosci. Abstr. 24, 431.11 (1998)
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999) Abstract
 
 
ALX-550-378 Revised 13-Jun-03
XE-CCG-I
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SYNONYMS UPF 711
(2S,1'S,2'S,3'R)-2-(2'-Carboxy-3'-(2-xanthylethyl)-cyclopropyl)glycine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-378-M001   1 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C21H21NO5
MW: 367.4
PURITY: ≥95%
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective and highly active group II mGluR antagonist with a subtype specificity towards the mGlu3 receptor. No activity towards group I and group III mGluRs.
Product Specific Literature References
Metabotropic glutamate receptors: new ligands and molecular modeling studies: R. Pellicciari, et al.; Neuropharmacology 38, A34 (1999)
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999) Abstract
 
 
ALX-550-380 Revised 06-Feb-05
PBDA
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SYNONYMS 4,4'-Phosphonicobis(butane-1,3-dicarboxylic acid)
PRODUCT LINE Neurobiology
PRODUCT CATEGORY NAALADase / Related Products
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ALX-550-380-M001   1 mg 55.00 USD Add To Cart
ALX-550-380-M005   5 mg 220.00 USD Add To Cart
Product Specification
FORMULA: C12H19O10P
MW: 354.3
PURITY: ≥95%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent inhibitor of glutamate carboxypeptidase II (NAAG peptidase) and an mGluR3-selective agonist.
Further Categories Containing This Product:
Glutamate Receptors (Metabotropic) / Related Products
 
 
ALX-550-381 Revised 23-May-06
MTEP
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SYNONYMS 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-381-M005   5 mg 75.00 USD Add To Cart
ALX-550-381-M025   25 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C11H8N2S
MW: 200.3
PURITY: ≥99%
APPEARANCE: White to yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent and highly selective antagonist for mGluR5^with a 5-fold higher anxiolytic activity than MPEP (Prod. No. ALX-550-368). Shows fewer off-target effects than MPEP.
Product Specific Literature References
[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization: J.J. Anderson, et al.; J. Pharmacol. Exp. Ther. 303, 1044 (2002) Abstract
Reduced stress-induced hyperthermia in mGluR5 knockout mice: J. Brodkin, et al.; Eur. J. Neurosci. 16, 2241 (2002) Abstract
[3H]-Methoxymethyl-MTEP and [3H]-Methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor: N.D. Cosford, et al.; Bioorg. Med. Chem. Lett. 13, 351 (2003) Abstract
Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling: A. Klodzinska, et al.; Neuropharmacology 47, 342 (2004) Abstract
Neuroprotective activity of the mGluR5 antagonists MPEP and MTEP against acute excitotoxicity differs and does not reflect actions at mGluR5 receptors: P.M.t. Lea, et al.; Br. J. Pharmacol. 145, 527 (2005) Abstract
MTEP, a new selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5), produces antiparkinsonian-like effects in rats: K. Ossowska, et al.; Neuropharmacology 49, 447 (2005) Abstract
Potential antidepressant-like effect of MTEP, a potent and highly selective mGluR5 antagonist: A. Palucha, et al.; Pharmacol. Biochem. Behav. 81, 901 (2005) Abstract
In vitro metabolic studies on the selective metabotropic glutamate receptor sub-type 5 (mGluR5) antagonist 3-[(2-methyl-1,3-thiazol-4-yl) ethynyl]-pyridine (MTEP): M.D. Green, et al.; Neurosci. Lett. 391, 91 (2006) Abstract
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Further Categories Containing This Product:
Anxiolytic Agents / Related Products
 
 
ALX-550-412 Revised 22-Apr-08
JNJ 16259685
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic) / Related Products
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ALX-550-412-M005   5 mg 80.00 USD Add To Cart
ALX-550-412-M025   25 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C20H23NO3
MW: 325.4
CAS NUMBER: 409345-29-5
PURITY: