Target Information
Target General Infomation | |||||
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Target ID |
T77548
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Former ID |
TTDR00755
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Target Name |
Metabotropic glutamate receptor 8
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Gene Name |
GRM8
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Synonyms |
Glutamate receptor mGLU8; MGLUR8; MGluR8a; GRM8
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Target Type |
Research
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Function |
Receptor for glutamate. The activity of this receptor is mediated by a g-protein that inhibits adenylate cyclase activity.
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BioChemical Class |
GPCR glutamate
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Target Validation |
T77548
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UniProt ID | |||||
Sequence |
MVCEGKRSASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGER
GVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFV QALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTA PELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISR EIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQS GHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFA EFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMH KDLCPGYIGLCPRMSTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQITN KSTEYKVIGHWTNQLHLKVEDMQWAHREHTHPASVCSLPCKPGERKKTVKGVPCCWHCER CEGYNYQVDELSCELCPLDQRPNMNRTGCQLIPIIKLEWHSPWAVVPVFVAILGIIATTF VIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRVFLGLGMC FSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPH IIIDYGEQRTLDPEKARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEA KPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYI IIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTY ISYSNHSI |
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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 525476 | Cloning 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 525723 | Constraints 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 525751 | Pharmacological 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 526630 | The metabotropic glutamate receptors: structure, activation mechanism and pharmacology. Curr Drug Targets CNS Neurol Disord. 2002 Jun;1(3):297-317. | ||||
Ref 527336 | Bioorg 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 528723 | Bioorg 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 530848 | Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav Brain Res. 2010 Oct 15;212(2):168-73. | ||||
Ref 534561 | Group 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. |
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