2-Metil-6-(feniletinil)piridin

Из Википедије, слободне енциклопедије
2-Metil-6-(feniletinil)piridin
Methylphenylethynylpyridine.png
IUPAC ime
2-Metil-6-(feniletinil)piridin
Identifikatori
CAS broj 96206-92-7 ДаY
ATC kod none
PubChem CID 3025961
IUPHAR/BPS 1426
ChemSpider 7970355 ДаY
Hemijski podaci
Formula C14H11N
Molarna masa 193,243 g/mol
  (verify)

2-Metil-6-(feniletinil)piridin (MPEP) je lek koji se koristi u naučnim istraživanjima. On je bio jedan od prvih selektivnih antagonista metabotropnog glutamatnog receptora mGluR5. Ovo jedinjenje je razvila farmaceutska kompanija Novartis krajem 1990-tih.[1] On proizvodi neuroprotektivne efekte nakon akutne moždane povrede u životinjskim ispitivanjima, mada nije jasno da li su ti rezultati direktna posledica mGluR5 blokade, jer on deluje i kao slab NMDA antagonist,[2][3] i kao pozitivni alosterni modulator mGlu4 receptora,[4] a isto tako postoje dokazi o funkcionalnim interakcijama između mGluR5 i NMDA receptora u pojedinim populacijama neurona.[5] Takođe je pokazano da proizvodi antidepresivne[6][7][8] i anksiolitičke efekte kod životinja,[9][10][11] i da umanjuje dejstvo morfinskog povlačenja,[12] najverovatnije usled direktne interakcije između mGluR5 i μ-opioidnog receptora.[13]

Reference[уреди]

  1. Micheli, F (2000). „Methylphenylethynylpyridine (MPEP) Novartis”. Current opinion in investigational drugs (London, England : 2000). 1 (3): 355—9. PMID 11249719. 
  2. O'Leary, DM; Movsesyan, V; Vicini, S; Faden, AI (2000). „Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antagonism”. British Journal of Pharmacology. 131 (7): 1429—37. doi:10.1038/sj.bjp.0703715. PMC 1572472слободно за читање. PMID 11090117. 
  3. Movsesyan, VA; O'Leary, DM; Fan, L; Bao, W; Mullins, PG; Knoblach, SM; Faden, AI (2001). „MGluR5 antagonists 2-methyl-6-(phenylethynyl)-pyridine and (E)-2-methyl-6-(2-phenylethenyl)-pyridine reduce traumatic neuronal injury in vitro and in vivo by antagonizing N-methyl-D-aspartate receptors”. The Journal of Pharmacology and Experimental Therapeutics. 296 (1): 41—7. PMID 11123360. 
  4. 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. doi:10.1038/sj.bjp.0705159. PMC 1573757слободно за читање. PMID 12684257. 
  5. Pisani, A; Gubellini, P; Bonsi, P; Conquet, F; Picconi, B; Centonze, D; Bernardi, G; Calabresi, P (2001). „Metabotropic glutamate receptor 5 mediates the potentiation of N-methyl-D-aspartate responses in medium spiny striatal neurons”. Neuroscience. 106 (3): 579—87. doi:10.1016/S0306-4522(01)00297-4. PMID 11591458. 
  6. Li, X; Need, AB; Baez, M; Witkin, JM (2006). „Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice”. The Journal of Pharmacology and Experimental Therapeutics. 319 (1): 254—9. doi:10.1124/jpet.106.103143. PMID 16803860. 
  7. Tatarczyńska, E; Klodzińska, A; Chojnacka-Wójcik, E; Palucha, A; Gasparini, F; Kuhn, R; Pilc, A (2001). „Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist”. British Journal of Pharmacology. 132 (7): 1423—30. doi:10.1038/sj.bjp.0703923. PMC 1572682слободно за читање. PMID 11264235. 
  8. Pilc, A; Kłodzińska, A; Brański, P; Nowak, G; Pałucha, A; Szewczyk, B; Tatarczyńska, E; Chojnacka-Wójcik, E; et al. (2002). „Multiple MPEP administrations evoke anxiolytic- and antidepressant-like effects in rats”. Neuropharmacology. 43 (2): 181—7. doi:10.1016/S0028-3908(02)00082-5. PMID 12213272. 
  9. Kłodzińska, A; Tatarczyńska, E; Chojnacka-Wójcik, E; Pilc, A (2000). „Anxiolytic-like effects of group I metabotropic glutamate antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) in rats”. Polish journal of pharmacology. 52 (6): 463—6. PMID 11334240. 
  10. Ballard, TM; Woolley, ML; Prinssen, E; Huwyler, J; Porter, R; Spooren, W (2005). „The effect of the mGlu5 receptor antagonist MPEP in rodent tests of anxiety and cognition: a comparison”. Psychopharmacology. 179 (1): 218—29. doi:10.1007/s00213-005-2211-9. PMID 15739074. 
  11. Varty, GB; Grilli, M; Forlani, A; Fredduzzi, S; Grzelak, ME; Guthrie, DH; Hodgson, RA; Lu, SX; et al. (2005). „The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy and side-effect profiles”. Psychopharmacology. 179 (1): 207—17. doi:10.1007/s00213-005-2143-4. PMID 15682298. 
  12. Rasmussen, K; Martin, H; Berger, JE; Seager, MA (2005). „The mGlu5 receptor antagonists MPEP and MTEP attenuate behavioral signs of morphine withdrawal and morphine-withdrawal-induced activation of locus coeruleus neurons in rats”. Neuropharmacology. 48 (2): 173—80. doi:10.1016/j.neuropharm.2004.09.010. PMID 15695156. 
  13. Schröder, H; Wu, DF; Seifert, A; Rankovic, M; Schulz, S; Höllt, V; Koch, T (2009). „Allosteric modulation of metabotropic glutamate receptor 5 affects phosphorylation, internalization, and desensitization of the micro-opioid receptor”. Neuropharmacology. 56 (4): 768—78. doi:10.1016/j.neuropharm.2008.12.010. PMID 19162047.