Metabotropic glutamate receptor 1: Difference between revisions
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==External links== |
==External links== |
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*{{cite web | url = http://www.iuphar-db.org/ |
*{{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2268 | title = Metabotropic Glutamate Receptors: mGlu<sub>1</sub> | accessdate = | author = | authorlink = | coauthors = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }} |
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==Further reading== |
==Further reading== |
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Revision as of 15:31, 5 December 2008
Template:PBB The glutamate receptor, metabotropic 1, also known as GRM1, is a human gene which encodes the metabotropic glutamate receptor 1 (mGluR1) protein.[1]
Ligands
In addition to the orthosteric site (the site where the endogenous ligand glutamate binds) at least two distinct allosteric binding sites exist on the mGluR1.[2] A respectable number of potent and specific allosteric ligands – predominantly antagonists/inhibitors – has been developed in recent years, although no orthosteric subtype-selective ligands have yet been discovered (2008).[3]
- JNJ-16259685: highly potent, selective non-competitive antagonist[4]
- R-214,127 and [3H]-analog: high-affinity, selective allosteric inhibitor[5]
- YM-202,074: high-affinity, selective allosteric antagonist[6]
- YM-230,888: high-affinity, selective allosteric antagonist[7]
- YM-298,198 and [3H]-analog: selective non-competitive antagonist[8]
- FTIDC: highly potent and selective allosteric antagonist/inverse agonist[9]
- A-841,720: potent non-competitive antagonist; minor hmGluR5 binding[10]
- VU-71: potentiator[11]
See also
References
- ^ "Entrez Gene: GRM1 glutamate receptor, metabotropic 1".
- ^ Hemstapat K, de Paulis T, Chen Y; et al. (2006). "A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators". Mol. Pharmacol. 70 (2): 616–26. doi:10.1124/mol.105.021857. PMID 16645124.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ based on a plain pubmed review
- ^ Lavreysen H, Wouters R, Bischoff F; et al. (2004). "JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist". Neuropharmacology. 47 (7): 961–72. doi:10.1016/j.neuropharm.2004.08.007. PMID 15555631.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Lavreysen H, Janssen C, Bischoff F, Langlois X, Leysen JE, Lesage AS (2003). "[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists". Mol. Pharmacol. 63 (5): 1082–93. PMID 12695537.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Kohara A, Takahashi M, Yatsugi S; et al. (2008). "Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models". Brain Res. 1191: 168–79. doi:10.1016/j.brainres.2007.11.035. PMID 18164695.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Kohara A, Nagakura Y, Kiso T; et al. (2007). "Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models". Eur. J. Pharmacol. 571 (1): 8–16. doi:10.1016/j.ejphar.2007.05.030. PMID 17597604.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Kohara A, Toya T, Tamura S; et al. (2005). "Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1". J. Pharmacol. Exp. Ther. 315 (1): 163–9. doi:10.1124/jpet.105.087171. PMID 15976016.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Suzuki G, Kimura T, Satow A; et al. (2007). "Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC)". J. Pharmacol. Exp. Ther. 321 (3): 1144–53. doi:10.1124/jpet.106.116574. PMID 17360958.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ El-Kouhen O, Lehto SG, Pan JB; et al. (2006). "Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist". Br. J. Pharmacol. 149 (6): 761–74. doi:10.1038/sj.bjp.0706877. PMID 17016515.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ Hemstapat K, de Paulis T, Chen Y; et al. (2006). "A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators". Mol. Pharmacol. 70 (2): 616–26. doi:10.1124/mol.105.021857. PMID 16645124.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link)
External links
- "Metabotropic Glutamate Receptors: mGlu1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
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Further reading
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.