Therapeutic Targets Database
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TTD Target ID: TTDC00220

Target Information
NameMetabotropic glutamate receptor 1    
Type of targetClinical trial target    
SynonymsGlutamate receptor mGLU1    
mGLUR1    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Convulsions
[ICD9: 780.3   ICD10: R56.0]
[1]
Neuronal injury[1]
Pain
[ICD9: 338,780   ICD10: R52, G89]
[1]
Drug(s)PF-1913539Phase IIIAlzheimer¡¯s Disease[2][3]
PF-1913539Phase IIIHuntington Disease[2][3]
AZD8529Phase IISchizophrenia[4]
AZD-9272Discontinued in Phase INeuropathic pain[5]
BioChemical ClassG-protein coupled receptor (metabotropic glutamate family)    
PathwayCalcium signaling pathway
Gap junction
Long-term depression
Long-term potentiation
Neuroactive ligand-receptor interaction
UniProt IDQ13255
FunctionReceptor for glutamate. The activity of this receptor is mediated by a g-protein that activates a phosphatidylinositol- calcium second messenger system. May participate in the central action of glutamate in the cns, such as long-term potentiation.    
SequenceMVGLLLFFFPAIFLEVSLLPRSPGRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAE KVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSI EFIRDSLISIRDEKDGINRCLPDGQSLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDI PQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESG MDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLL SAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLD TNTRNPWFPEFWQHRFQCRLPGHLLENPNFKRICTGNESLEENYVQDSKMGFVINAIYAM AHGLQNMHHALCPGHVGLCDAMKPIDGSKLLDFLIKSSFIGVSGEEVWFDEKGDAPGRYD IMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGVVRSVCSEPCLKGQIKVIRKGE VSCCWICTACKENEYVQDEFTCKACDLGWWPNADLTGCEPIPVRYLEWSNIESIIAIAFS CLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQ RLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTL VVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPLGYNGLLIMSCTYYAFKTRNVPAN FNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIA KPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKAGAGNANSNGKSVSWSEPGG GQVPKGQHMWHRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDTSTKTLYNVEEE EDAQPIRFSPPGSPSMVVHRRVPSAATTPPLPPHLTAEETPLFLAEPALPKGLPPPLQQQ QQPPPQQKSLMDQLQGVVSNFSTAIPDFHAVLAGPGGPGNGLRSLYPPPPPPQHLQMLPL QLSTFGEELVSPPADDDDDSERFKLLQEYVYEHEREGNTEEDELEEEEEDLQAASKLTPD DSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVSYASVILRDYKQSSSTL
Related US Patent6,482,824
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3,4-dimethylphenyl)[6]
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone[6]
(E)-4,4-Dimethyl-1-quinolin-3-yl-pent-1-en-3-one[6]
2-methyl-6- (phenylethynyl)pyridine[7]
4- (1-Amino-1-Carboxy-Ethyl)-Benzoic Acid[8]
4- (cyclohexyloxy)quinazoline[9]
6-bromo-N- (3-chlorophenyl)quinazolin-4-amine[10]
GLUTAMATE[11]
JNJ-16259685[12]
N- (2,3-dihydro-1H-inden-2-yl)isoquinolin-1-amine[9]
N- (2,3-dihydro-1H-inden-2-yl)quinazolin-4-amine[9]
N- (2-methyl-2-phenylpropyl)pyrazine-2-carboxamide[13]
N- (2-phenylpropyl)quinoxaline-2-carboxamide[13]
N- (3-bromophenyl)-6-chloroquinazolin-4-amine[10]
N- (3-bromophenyl)-6-fluoroquinazolin-4-amine[10]
N-cyclohexylquinazolin-4-amine[9]
N-cyclohexylquinolin-4-amine[9]
N-phenethylquinoxaline-2-carboxamide[13]
QUISQUALATE[14]
VU0080241[15]
pyrazine-2-carboxylic acid adamantan-1-ylamide[16]
quinoline-2-carboxylic acid adamantan-1-ylamide[16]
quinoline-3-carboxylic acid adamantan-1-ylamide[16]
quinoxaline-2-carboxylic acid adamantan-1-ylamide[16]
AgonistAZD8529[4]
AntagonistPF-1913539[2][3]
ModulatorAZD-9272[5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol. 2002 Feb;2(1):43-9. To Reference
Ref 2Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 3Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med. 2003 Nov;136(5):474-7. To Reference
Ref 4AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 5Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 6Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. Epub 2009 Jun 23.Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1. To Reference
Ref 7Bioorg Med Chem Lett. 2010 Aug 1;20(15):4371-5. Epub 2010 Jun 17.Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists. To Reference
Ref 8Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 9Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. Epub 2009 Mar 3.In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists. To Reference
Ref 10Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. To Reference
Ref 11J Med Chem. 2007 Sep 20;50(19):4630-41. Epub 2007 Aug 29.Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs. To Reference
Ref 12J Med Chem. 2007 May 31;50(11):2563-8. Epub 2007 May 10.Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain. To Reference
Ref 13Bioorg Med Chem Lett. 2007 Jan 15;17(2):486-90. Epub 2006 Oct 11.Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain. To Reference
Ref 14J Med Chem. 1998 Mar 12;41(6):930-9.Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid. To Reference
Ref 15Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. Epub 2008 Aug 29.Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. To Reference
Ref 16J Med Chem. 2008 Feb 14;51(3):634-47. Epub 2008 Jan 4.Positive and negative modulation of group I metabotropic glutamate receptors. To Reference



 

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