Target Information
Target General Information | Top | |||||
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Target ID |
T27137
(Former ID: TTDC00220)
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Target Name |
Metabotropic glutamate receptor 1 (mGluR1)
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Synonyms |
mGLUR1; Glutamate receptor mGLU1; GPRC1A
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Gene Name |
GRM1
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Target Type |
Discontinued target
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[1] | ||||
Disease | [+] 6 Target-related Diseases | + | ||||
1 | Alzheimer disease [ICD-11: 8A20] | |||||
2 | Schizophrenia [ICD-11: 6A20] | |||||
3 | General pain disorder [ICD-11: 8E43] | |||||
4 | Cerebral ischaemia [ICD-11: 8B1Z] | |||||
5 | Pain [ICD-11: MG30-MG3Z] | |||||
6 | Dissociative neurological symptom disorder [ICD-11: 6B60] | |||||
Function |
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling activates a phosphatidylinositol-calcium second messenger system. May participate in the central action of glutamate in the CNS, such as long-term potentiation in the hippocampus and long-term depression in the cerebellum. G-protein coupled receptor for glutamate.
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BioChemical Class |
GPCR glutamate
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UniProt ID | ||||||
Sequence |
MVGLLLFFFPAIFLEVSLLPRSPGRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAE
KVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSI EFIRDSLISIRDEKDGINRCLPDGQSLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDI PQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESG MDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLL SAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLD TNTRNPWFPEFWQHRFQCRLPGHLLENPNFKRICTGNESLEENYVQDSKMGFVINAIYAM AHGLQNMHHALCPGHVGLCDAMKPIDGSKLLDFLIKSSFIGVSGEEVWFDEKGDAPGRYD IMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGVVRSVCSEPCLKGQIKVIRKGE VSCCWICTACKENEYVQDEFTCKACDLGWWPNADLTGCEPIPVRYLEWSNIESIIAIAFS CLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQ RLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTL VVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPLGYNGLLIMSCTYYAFKTRNVPAN FNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIA KPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKAGAGNANSNGKSVSWSEPGG GQVPKGQHMWHRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDTSTKTLYNVEEE EDAQPIRFSPPGSPSMVVHRRVPSAATTPPLPSHLTAEETPLFLAEPALPKGLPPPLQQQ QQPPPQQKSLMDQLQGVVSNFSTAIPDFHAVLAGPGGPGNGLRSLYPPPPPPQHLQMLPL QLSTFGEELVSPPADDDDDSERFKLLQEYVYEHEREGNTEEDELEEEEEDLQAASKLTPD DSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVSYASVILRDYKQSSSTL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T02U6A |
Drugs and Modes of Action | Top | |||||
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Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
1 | PF-1913539 | Drug Info | Discontinued in Phase 3 | Alzheimer disease | [2] | |
2 | AZD8529 | Drug Info | Discontinued in Phase 2 | Schizophrenia | [3], [4] | |
3 | AZD-9272 | Drug Info | Discontinued in Phase 1 | Neuropathic pain | [5], [6] | |
4 | LY-367385 | Drug Info | Terminated | Neurological disorder | [11], [12] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | A-841720 | Drug Info | Preclinical | Pain | [7], [8] | |
2 | NPS-2390 | Drug Info | Preclinical | Cerebrovascular ischaemia | [9], [10] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Antagonist | [+] 9 Antagonist drugs | + | ||||
1 | PF-1913539 | Drug Info | [13], [14] | |||
2 | A-841720 | Drug Info | [1] | |||
3 | (+)-MCPG | Drug Info | [18], [19] | |||
4 | (S)-(+)-CBPG | Drug Info | [22] | |||
5 | (S)-4C3HPG | Drug Info | [20] | |||
6 | (S)-4CPG | Drug Info | [18] | |||
7 | (S)-TBPG | Drug Info | [23] | |||
8 | 3-MATIDA | Drug Info | [26] | |||
9 | AIDA | Drug Info | [18] | |||
Agonist | [+] 8 Agonist drugs | + | ||||
1 | AZD8529 | Drug Info | [15] | |||
2 | LY-367385 | Drug Info | [17] | |||
3 | (1S,3R)-ACPD | Drug Info | [20] | |||
4 | (S)-3HPG | Drug Info | [20] | |||
5 | 3,5-DHPG | Drug Info | [18] | |||
6 | ibotenate | Drug Info | [20] | |||
7 | L-CCG-I | Drug Info | [20] | |||
8 | [3H]quisqualate | Drug Info | [57], [58] | |||
Modulator | [+] 2 Modulator drugs | + | ||||
1 | AZD-9272 | Drug Info | [6] | |||
2 | LY-3390334 | Drug Info | [36] | |||
Inhibitor | [+] 20 Inhibitor drugs | + | ||||
1 | NPS-2390 | Drug Info | [16] | |||
2 | (3,4-dimethylphenyl)(4-phenoxyphenyl)methanone | Drug Info | [21] | |||
3 | (E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone | Drug Info | [21] | |||
4 | (E)-4,4-Dimethyl-1-quinolin-3-yl-pent-1-en-3-one | Drug Info | [21] | |||
5 | 2-methyl-6-(phenylethynyl)pyridine | Drug Info | [24] | |||
6 | 4-(cyclohexyloxy)quinazoline | Drug Info | [27] | |||
7 | 6-bromo-N-(3-chlorophenyl)quinazolin-4-amine | Drug Info | [28] | |||
8 | N-(2,3-dihydro-1H-inden-2-yl)isoquinolin-1-amine | Drug Info | [27] | |||
9 | N-(2,3-dihydro-1H-inden-2-yl)quinazolin-4-amine | Drug Info | [27] | |||
10 | N-(2-methyl-2-phenylpropyl)pyrazine-2-carboxamide | Drug Info | [39] | |||
11 | N-(2-phenylpropyl)quinoxaline-2-carboxamide | Drug Info | [39] | |||
12 | N-(3-bromophenyl)-6-chloroquinazolin-4-amine | Drug Info | [28] | |||
13 | N-(3-bromophenyl)-6-fluoroquinazolin-4-amine | Drug Info | [28] | |||
14 | N-cyclohexylquinazolin-4-amine | Drug Info | [27] | |||
15 | N-cyclohexylquinolin-4-amine | Drug Info | [27] | |||
16 | N-phenethylquinoxaline-2-carboxamide | Drug Info | [39] | |||
17 | Pyrazine-2-carboxylic acid adamantan-1-ylamide | Drug Info | [16] | |||
18 | Quinoline-2-carboxylic acid adamantan-1-ylamide | Drug Info | [16] | |||
19 | Quinoline-3-carboxylic acid adamantan-1-ylamide | Drug Info | [16] | |||
20 | VU0080241 | Drug Info | [50] | |||
Modulator (allosteric modulator) | [+] 51 Modulator (allosteric modulator) drugs | + | ||||
1 | 3,5-dimethyl PPP | Drug Info | [25] | |||
2 | A-794278 | Drug Info | [29] | |||
3 | A-794282 | Drug Info | [29] | |||
4 | A-850002 | Drug Info | [29] | |||
5 | BAY 367620 | Drug Info | [30] | |||
6 | CFMMC | Drug Info | [31] | |||
7 | CFMTI | Drug Info | [32] | |||
8 | CPCCOEt | Drug Info | [18] | |||
9 | DM-PPP | Drug Info | [25] | |||
10 | FPTQ | Drug Info | [33] | |||
11 | FTIDC | Drug Info | [34] | |||
12 | JNJ-16567083 | Drug Info | [35] | |||
13 | LY456066 | Drug Info | [31] | |||
14 | LY456236 | Drug Info | [37] | |||
15 | MK-5435 | Drug Info | [38] | |||
16 | PHCCC | Drug Info | [37] | |||
17 | PMID12470711C3 | Drug Info | [25] | |||
18 | PMID16099654C3a | Drug Info | [40] | |||
19 | PMID16099654C4b | Drug Info | [40] | |||
20 | PMID17064898C29 | Drug Info | [39] | |||
21 | PMID17276684C22 | Drug Info | [41] | |||
22 | PMID17532216C2f | Drug Info | [42] | |||
23 | PMID17929793C11c | Drug Info | [43] | |||
24 | PMID17929793C23c | Drug Info | [43] | |||
25 | PMID17929793C23e | Drug Info | [43] | |||
26 | PMID17929793C23h | Drug Info | [43] | |||
27 | PMID17929793C23i | Drug Info | [43] | |||
28 | PMID19289283C22 | Drug Info | [27] | |||
29 | PMID19289283C32 | Drug Info | [27] | |||
30 | PMID19433355C11q | Drug Info | [44] | |||
31 | PMID19433355C11s | Drug Info | [44] | |||
32 | PMID20346665C24 | Drug Info | [45] | |||
33 | PMID20346665C27 | Drug Info | [45] | |||
34 | PMID22266036C12e | Drug Info | [46] | |||
35 | PMID22266036C9a | Drug Info | [46] | |||
36 | PMID23084894C10i | Drug Info | [47] | |||
37 | PMID23084894C9n | Drug Info | [47] | |||
38 | R214127 | Drug Info | [18] | |||
39 | Ro01-6128 | Drug Info | [48] | |||
40 | Ro0711401 | Drug Info | [49] | |||
41 | Ro67-4853 | Drug Info | [48] | |||
42 | Ro67-7476 | Drug Info | [48] | |||
43 | VU-71 | Drug Info | [40] | |||
44 | VU0469650 | Drug Info | [51] | |||
45 | YM-202074 | Drug Info | [52] | |||
46 | YM298198 | Drug Info | [53] | |||
47 | [11C]MMTP | Drug Info | [54] | |||
48 | [18F]FITM | Drug Info | [55] | |||
49 | [18F]FPIT | Drug Info | [56] | |||
50 | [18F]MK-1312 | Drug Info | [38] | |||
51 | [3H]EM-TBPC | Drug Info | [57] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 9 KEGG Pathways | + | ||||
1 | Calcium signaling pathway | |||||
2 | FoxO signaling pathway | |||||
3 | Neuroactive ligand-receptor interaction | |||||
4 | Gap junction | |||||
5 | Long-term potentiation | |||||
6 | Retrograde endocannabinoid signaling | |||||
7 | Glutamatergic synapse | |||||
8 | Long-term depression | |||||
9 | Estrogen signaling pathway | |||||
Panther Pathway | [+] 4 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
2 | Metabotropic glutamate receptor group III pathway | |||||
3 | Metabotropic glutamate receptor group I pathway | |||||
4 | Endogenous cannabinoid signaling | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | G alpha (q) signalling events | |||||
2 | Class C/3 (Metabotropic glutamate/pheromone receptors) | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | Hypothetical Network for Drug Addiction | |||||
2 | GPCRs, Class C Metabotropic glutamate, pheromone | |||||
3 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
4 | GPCR ligand binding | |||||
5 | GPCR downstream signaling | |||||
6 | GPCRs, Other |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Comparison of the mGluR1 antagonist A-841720 in rat models of pain and cognition. Behav Pharmacol. 2007 Jul;18(4):273-81. | |||||
REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021875) | |||||
REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7678). | |||||
REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029661) | |||||
REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6439). | |||||
REF 6 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3953). | |||||
REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024545) | |||||
REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1384). | |||||
REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014988) | |||||
REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1379). | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011092) | |||||
REF 13 | Pfizer. Product Development Pipeline. March 31 2009. | |||||
REF 14 | Comparative 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. | |||||
REF 15 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
REF 16 | Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem. 2008 Feb 14;51(3):634-47. | |||||
REF 17 | Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur J Pharmacol. 1999 Feb 26;368(1):17-24. | |||||
REF 18 | [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. Mol Pharmacol. 2003 May;63(5):1082-93. | |||||
REF 19 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
REF 20 | Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J Neurochem. 2000 Dec;75(6):2590-601. | |||||
REF 21 | Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate recepto... Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. | |||||
REF 22 | Biochemical and electrophysiological studies on (S)-(+)-2-(3'-carboxybicyclo(1.1.1)pentyl)-glycine (CBPG), a novel mGlu5 receptor agonist endowed with mGlu1 receptor antagonist activity. Neuropharmacology. 1999 Jul;38(7):917-26. | |||||
REF 23 | Synthesis and biological evaluation of 2-(3'-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist. Bioorg Med Chem. 2001 Feb;9(2):221-7. | |||||
REF 24 | Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4371-5. | |||||
REF 25 | Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists. Bioorg Med Chem. 2003 Jan 17;11(2):171-83. | |||||
REF 26 | The novel and systemically active metabotropic glutamate 1 (mGlu1) receptor antagonist 3-MATIDA reduces post-ischemic neuronal death. Neuropharmacology. 2002 May;42(6):741-51. | |||||
REF 27 | In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4. | |||||
REF 28 | Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. | |||||
REF 29 | Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. J Med Chem. 2005 Nov 17;48(23):7374-88. | |||||
REF 30 | BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. Mol Pharmacol. 2001 May;59(5):965-73. | |||||
REF 31 | Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one. Neuropharmacology. 2009 Sep;57(4):438-45. | |||||
REF 32 | Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one. J Pharmacol Exp Ther. 2009 Jul;330(1):179-90. | |||||
REF 33 | Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain. Bioorg Med Chem. 2011 Jan 1;19(1):102-10. | |||||
REF 34 | Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-... J Pharmacol Exp Ther. 2007 Jun;321(3):1144-53. | |||||
REF 35 | A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone. J Med Chem. 2005 Aug11;48(16):5096-9. | |||||
REF 36 | Inhibition of group I metabotropic glutamate receptor responses in vivo in rats by a new generation of carboxyphenylglycine-like amino acid antagon... Neurosci Lett. 2002 Sep 20;330(2):127-30. | |||||
REF 37 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 289). | |||||
REF 38 | Synthesis, characterization, and monkey PET studies of [ ]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435. Synapse. 2011 Feb;65(2):125-35. | |||||
REF 39 | Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain. Bioorg Med Chem Lett. 2007 Jan 15;17(2):486-90. | |||||
REF 40 | 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4628-31. | |||||
REF 41 | From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2254-9. | |||||
REF 42 | Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4303-7. | |||||
REF 43 | Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain. J Med Chem. 2007 Nov 15;50(23):5550-3. | |||||
REF 44 | Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3199-203. | |||||
REF 45 | A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2474-7. | |||||
REF 46 | Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1575-8. | |||||
REF 47 | Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7223-6. | |||||
REF 48 | Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7. | |||||
REF 49 | Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1666-9. | |||||
REF 50 | Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel ... Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. | |||||
REF 51 | N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. | |||||
REF 52 | Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models. Brain Res. 2008 Jan 29;1191:168-79. | |||||
REF 53 | Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide ... J Pharmacol Exp Ther. 2005 Oct;315(1):163-9. | |||||
REF 54 | Synthesis, in vitro and in vivo evaluation of [11C]MMTP: a potential PET ligand for mGluR1 receptors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3499-501. | |||||
REF 55 | Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1. Bioorg Med Chem Lett. 2011 May 15;21(10):2998-3001. | |||||
REF 56 | Characterization of 1-(2-[18F] fluoro-3-pyridyl)-4-(2-isopropyl-1-oxo- isoindoline-5-yl)-5-methyl-1H-1,2,3-triazole, a PET ligand for imaging the metabotropic glutamate receptor type 1 in rat and monkey brains. J Neurochem. 2012 Apr;121(1):115-24. | |||||
REF 57 | Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glut... J Biol Chem. 2003 Mar 7;278(10):8340-7. | |||||
REF 58 | Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)... J Med Chem. 1998 Mar 12;41(6):930-9. |
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