Target Information

Target General Infomation
Target ID
T77548
Former ID
TTDR00755
Target Name
Metabotropic glutamate receptor 8
Gene Name
GRM8
Synonyms
Glutamate receptor mGLU8; MGLUR8; MGluR8a; GRM8
Target Type
Research
Function
Receptor for glutamate. The activity of this receptor is mediated by a g-protein that inhibits adenylate cyclase activity.
BioChemical Class
GPCR glutamate
Target Validation
T77548
UniProt ID
O00222
Sequence
MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGER
GVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFV
QALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTA
PELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISR
EIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQS
GHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFA
EFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMH
KDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITN
KSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCER
CEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTF
VIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMC
FSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPH
IIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEA
KPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYI
IIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTY
ISYSNHSI
Agonist (1S,3R)-ACPD Drug Info [534561]
(R,S)-4-phosphonophenylglycine Drug Info [534919]
(S)-3,4-DCPG Drug Info [525960]
ACPT-I Drug Info [525751]
D-AP4 Drug Info [534561]
L-AP4 Drug Info [525476]
L-CCG-I Drug Info [525476]
L-serine-O-phosphate Drug Info [525476]
[3H]AP4 Drug Info [525476]
Inhibitor 2-Amino-4-phosphono-butyric acid Drug Info [527336]
GLUTAMATE Drug Info [528723]
L-1-amino-4-phosphonobutanoic acid Drug Info [528723]
QUISQUALATE Drug Info [534590]
Antagonist alpha-methylserine-O-phosphate Drug Info [526630]
CPPG Drug Info [525723]
MAP4 Drug Info [525723]
MPPG Drug Info [534561]
Modulator (allosteric modulator) AZ12216052 Drug Info [530848]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Glutamatergic synapse
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Metabotropic glutamate receptor group III pathway
Reactome G alpha (i) signalling events
Class C/3 (Metabotropic glutamate/pheromone receptors)
WikiPathways GPCRs, Class C Metabotropic glutamate, pheromone
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 525476Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8. Brain Res Mol Brain Res. 1999 Apr 20;67(2):201-10.
Ref 525723Constraints on proper folding of the amino terminal domains of group III metabotropic glutamate receptors. Brain Res Mol Brain Res. 2000 Mar 10;76(1):180-90.
Ref 525751Pharmacological characterization of the rat metabotropic glutamate receptor type 8a revealed strong similarities and slight differences with the type 4a receptor. Eur J Pharmacol. 2000 Apr 7;394(1):17-26.
Ref 525960(S)-3,4-DCPG, a potent and selective mGlu8a receptor agonist, activates metabotropic glutamate receptors on primary afferent terminals in the neonatal rat spinal cord. Neuropharmacology. 2001 Mar;40(3):311-8.
Ref 526630The metabotropic glutamate receptors: structure, activation mechanism and pharmacology. Curr Drug Targets CNS Neurol Disord. 2002 Jun;1(3):297-317.
Ref 527336Bioorg Med Chem Lett. 2005 Jan 17;15(2):349-51.(2S,1'S,2'R,3'R)-2(2'-Carboxy-3'-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors.
Ref 528723Bioorg Med Chem. 2007 May 1;15(9):3161-70. Epub 2007 Feb 22.Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.
Ref 530848Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav Brain Res. 2010 Oct 15;212(2):168-73.
Ref 534561Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells. Brain Res Mol Brain Res. 1998 Jan;53(1-2):88-97.
Ref 534590J 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.
Ref 534919Anticonvulsant activity of a metabotropic glutamate receptor 8 preferential agonist, (R,S)-4-phosphonophenylglycine. Eur J Pharmacol. 1999 Oct 21;383(1):23-7.

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