SIB-1757: Difference between revisions

{{drugbox

| IUPAC_name = 6-methyl-2-(phenylazo)-3-pyridinol

| image = SIB-1757_structure.png

| width = 200

| CAS_number = 31993-01-8

| ATC_prefix =

| ATC_suffix =

| PubChem = 6849066

| DrugBank =

| C=12|H=11|N=3|O=1

| molecular_weight = 213.235 g/mol

| smiles = Oc1ccc(C)nc1\N=N\c2ccccc2

| bioavailability =

| protein_bound =

| metabolism =

| elimination_half-life =

| excretion =

| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->

| pregnancy_US = <!-- A / B / C / D / X -->

| pregnancy_category=

| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->

| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII -->

| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C -->

| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->

| legal_status =

| routes_of_administration =

}}

'''SIB-1757''' is a drug used in scientific research which was one of the first compounds developed that acts as a selective [[Antagonist (pharmacology)|antagonist]] for the [[metabotropic glutamate receptor]] subtype [[Metabotropic glutamate receptor 5|mGluR₅]].<ref name="pmid10381773">{{cite journal |author=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 |year=1999 |month=July |pmid=10381773 |doi= |url=}}</ref> It has anti-[[hyperalgesia]] effects in animals.<ref name="pmid10998562">{{cite journal |author=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 |year=2000 |month=October |pmid=10998562 |doi= 10.1016/S0304-3940(00)01458-0|url=}}</ref> SIB-1757 along with other mGluR₅ antagonists has been shown to have neuroprotective and hepatoprotective effects,<ref name="pmid12547406">{{cite journal |author=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 |year=2003 |month=February |pmid=12547406 |doi= 10.1016/S0168-8278(02)00384-7|url=}}</ref><ref name="pmid12950444">{{cite journal |author=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 |year=2003 |month=September |pmid=12950444 |doi= 10.1046/j.1471-4159.2003.01932.x|url=}}</ref> and it is also used to study the role of the mGluR₅ receptor in brain development.<ref name="pmid16005029">{{cite journal |author=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=}}</ref>

== References ==

{{reflist}}

{{Glutamate_receptor_ligands}}

{{pharm-stub}}