| 词条 | SIB-1757 |
| 释义 |
| Watchedfields = changed | verifiedrevid = 417966671 | IUPAC_name = 6-methyl-2-(phenylazo)-3-pyridinol | image = SIB-1757_structure.png | width = 200 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 31993-01-8 | ATC_prefix = | ATC_suffix = | PubChem = 6849066 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID = 10654582 | C=12 | H=11 | N=3 | O=1 | molecular_weight = 213.235 g/mol | smiles = Oc1ccc(C)nc1\=N\\c2ccccc2 | StdInChI = 1S/C12H11N3O/c1-9-7-8-11(16)12(13-9)15-14-10-5-3-2-4-6-10/h2-8,16H,1H3/b15-14+ | StdInChIKey = LOCPVWIREQIGNQ-CCEZHUSRSA-N }}SIB-1757 is a drug used in scientific research which was one of the first compounds developed that acts as a selective antagonist for the metabotropic glutamate receptor subtype mGluR5.[1] It has anti-hyperalgesia effects in animals.[2] SIB-1757 along with other mGluR5 antagonists has been shown to have neuroprotective and hepatoprotective effects,[3][4] and it is also used to study the role of the mGluR5 receptor in brain development.[5] References1. ^{{cite journal |vauthors=Varney MA, Cosford ND, Jachec C, Rao SP, Sacaan A, Lin FF, Bleicher L, Santori EM, Flor PJ, Allgeier H, Gasparini F, Kuhn R, Hess SD, Veliçelebi G, Johnson EC |title=SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5 |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=290 |issue=1 |pages=170–81 |date=July 1999 |pmid=10381773 |doi= |url=}} {{Metabotropic glutamate receptor modulators}}{{nervous-system-drug-stub}}2. ^{{cite journal |vauthors=Dogrul A, Ossipov MH, Lai J, Malan TP, Porreca F |title=Peripheral and spinal antihyperalgesic activity of SIB-1757, a metabotropic glutamate receptor (mGLUR(5)) antagonist, in experimental neuropathic pain in rats |journal=Neuroscience Letters |volume=292 |issue=2 |pages=115–8 |date=October 2000 |pmid=10998562 |doi= 10.1016/S0304-3940(00)01458-0|url=}} 3. ^{{cite journal |vauthors=Storto M, Ngomba RT, Battaglia G, Freitas I, Griffini P, Richelmi P, Nicoletti F, Vairetti M |title=Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice |journal=Journal of Hepatology |volume=38 |issue=2 |pages=179–87 |date=February 2003 |pmid=12547406 |doi= 10.1016/S0168-8278(02)00384-7|url=}} 4. ^{{cite journal |vauthors=Fazal A, Parker F, Palmer AM, Croucher MJ |title=Characterisation of the actions of group I metabotropic glutamate receptor subtype selective ligands on excitatory amino acid release and sodium-dependent re-uptake in rat cerebrocortical minislices |journal=Journal of Neurochemistry |volume=86 |issue=6 |pages=1346–58 |date=September 2003 |pmid=12950444 |doi= 10.1046/j.1471-4159.2003.01932.x|url=}} 5. ^{{cite journal |vauthors=Bonsi P, Cuomo D, De Persis C, Centonze D, Bernardi G, Calabresi P, Pisani A |title=Modulatory action of metabotropic glutamate receptor (mGluR) 5 on mGluR1 function in striatal cholinergic interneurons |journal=Neuropharmacology |volume=Suppl 1 |issue= |pages=104–13 |series=49 |year=2005 |pmid=16005029 |doi=10.1016/j.neuropharm.2005.05.012 |url=}} 3 : Pyridines|Azo compounds|MGlu5 receptor antagonists |
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