SIB-1893
SIB-1893 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.[1] On ima antikonvulsivno i neuroprotektivno dejstvo,[2] i redukuje otpuštanje glutamata.[3] On takođe deluje kao pozitivni alosterni modulator mGluR4 receptora.[4]
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| IUPAC ime | |
|---|---|
(E)-2-metil-6-(2-feniletenil)piridin | |
| Identifikatori | |
| CAS broj | 6266-99-5  |
| ATC kod | none |
| PubChem | CID 235382 |
| ChEMBL | CHEMBL88612 |
| Hemijski podaci | |
| Formula | C14H13N |
| Molarna masa | 195,259 g/mol |
| |
Reference уреди
- ^ 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 (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.
- ^ Chapman AG, Nanan K, Williams M, Meldrum BS (2000). „Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893)”. Neuropharmacology. 39 (9): 1567—74. PMID 10854901. doi:10.1016/S0028-3908(99)00242-7.
- ^ Wang SJ, Sihra TS (2004). „Noncompetitive metabotropic glutamate5 receptor antagonist (E)-2-methyl-6-styryl-pyridine (SIB1893) depresses glutamate release through inhibition of voltage-dependent Ca2+ entry in rat cerebrocortical nerve terminals (synaptosomes)”. The Journal of Pharmacology and Experimental Therapeutics. 309 (3): 951—8. PMID 14982967. doi:10.1124/jpet.103.064881.
- ^ Mathiesen JM, Svendsen N, Bräuner-Osborne H, Thomsen C, Ramirez MT (2003). „Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP”. British Journal of Pharmacology. 138 (6): 1026—30. PMC 1573757
. PMID 12684257. doi:10.1038/sj.bjp.0705159.
