SIB-1757

SIB-1757
(IUPAC) ime
	6-metil-2-(fenilazo)-3-piridinol
Klinički podaci
Identifikatori
CAS broj	31993-01-8
ATC kod	nije dodeljen
PubChem	6849066
Hemijski podaci
Formula	C12H11N3O
Mol. masa	213,235 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=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+ ; Key: LOCPVWIREQIGNQ-CCEZHUSRSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

SIB-1757 je lek koji se koristi u naučnim istraživanjima. On je bio jedan od prvih jedinjenja razvijenih kao selektivni antagonisti za metabotropni glutamatni receptor podtip mGluR₅.^[3] On ima antihipergleziono dejstvo kod životinja.^[4] SIB-1757 zajedno sa drugim mGluR₅ antagonistima ima neuroprotektivne i hepatoprotektivne efekte,^[5]^[6] i on se takođe koristi u studiranju uloge mGluR₅ receptora tokom moždanog razvoja.^[7]

Reference uredi

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ 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 (July 1999). „SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5”. The Journal of Pharmacology and Experimental Therapeutics 290 (1): 170–81. PMID 10381773.
↑ Dogrul A, Ossipov MH, Lai J, Malan TP, Porreca F (October 2000). „Peripheral and spinal antihyperalgesic activity of SIB-1757, a metabotropic glutamate receptor (mGLUR(5)) antagonist, in experimental neuropathic pain in rats”. Neuroscience Letters 292 (2): 115–8. DOI:10.1016/S0304-3940(00)01458-0. PMID 10998562.
↑ Storto M, Ngomba RT, Battaglia G, Freitas I, Griffini P, Richelmi P, Nicoletti F, Vairetti M (February 2003). „Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice”. Journal of Hepatology 38 (2): 179–87. DOI:10.1016/S0168-8278(02)00384-7. PMID 12547406.
↑ Fazal A, Parker F, Palmer AM, Croucher MJ (September 2003). „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 of Neurochemistry 86 (6): 1346–58. DOI:10.1046/j.1471-4159.2003.01932.x. PMID 12950444.
↑ Bonsi P, Cuomo D, De Persis C, Centonze D, Bernardi G, Calabresi P, Pisani A (2005). „Modulatory action of metabotropic glutamate receptor (mGluR) 5 on mGluR1 function in striatal cholinergic interneurons”. Neuropharmacology. 49 Suppl 1: 104–13. DOI:10.1016/j.neuropharm.2005.05.012. PMID 16005029.

Spoljašnje veze uredi

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[pmid10381773-3] 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 (July 1999). „SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5”. The Journal of Pharmacology and Experimental Therapeutics 290 (1): 170–81. PMID 10381773.

[pmid10998562-4] Dogrul A, Ossipov MH, Lai J, Malan TP, Porreca F (October 2000). „Peripheral and spinal antihyperalgesic activity of SIB-1757, a metabotropic glutamate receptor (mGLUR(5)) antagonist, in experimental neuropathic pain in rats”. Neuroscience Letters 292 (2): 115–8. DOI:10.1016/S0304-3940(00)01458-0. PMID 10998562.

[pmid12547406-5] Storto M, Ngomba RT, Battaglia G, Freitas I, Griffini P, Richelmi P, Nicoletti F, Vairetti M (February 2003). „Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice”. Journal of Hepatology 38 (2): 179–87. DOI:10.1016/S0168-8278(02)00384-7. PMID 12547406.

[pmid12950444-6] Fazal A, Parker F, Palmer AM, Croucher MJ (September 2003). „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 of Neurochemistry 86 (6): 1346–58. DOI:10.1046/j.1471-4159.2003.01932.x. PMID 12950444.

[pmid16005029-7] Bonsi P, Cuomo D, De Persis C, Centonze D, Bernardi G, Calabresi P, Pisani A (2005). „Modulatory action of metabotropic glutamate receptor (mGluR) 5 on mGluR1 function in striatal cholinergic interneurons”. Neuropharmacology. 49 Suppl 1: 104–13. DOI:10.1016/j.neuropharm.2005.05.012. PMID 16005029.

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