2-Metil-6-(feniletinil)piridin

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2-Metil-6-(feniletinil)piridin
(IUPAC) ime
2-Metil-6-(feniletinil)piridin
Klinički podaci
Identifikatori
CAS broj 96206-92-7
ATC kod nije dodeljen
PubChem[1][2] 3025961
ChemSpider[3] 7970355
Hemijski podaci
Formula C14H11N 
Mol. masa 193,243 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

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.[4] 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,[5][6] i kao pozitivni alosterni modulator mGlu4 receptora,[7] a isto tako postoje dokazi o funkcionalnim interakcijama između mGluR5 i NMDA receptora u pojedinim populacijama neurona.[8] Takođe je pokazano da proizvodi antidepresivne[9][10][11] i anksiolitičke efekte kod životinja,[12][13][14] i da umanjuje dejstvo morfinskog povlačenja,[15] najverovatnije usled direktne interakcije između mGluR5 i μ-opioidnog receptora.[16]

Reference

[uredi | uredi kod]
  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. 
  3. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ Micheli, F (2000). „Methylphenylethynylpyridine (MPEP) Novartis”. Current opinion in investigational drugs (London, England : 2000) 1 (3): 355–9. PMID 11249719. 
  5. ↑ 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 1572472. PMID 11090117. 
  6. ↑ 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. 
  7. ↑ 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 1573757. PMID 12684257. 
  8. ↑ 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. 
  9. ↑ 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. 
  10. ↑ 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 1572682. PMID 11264235. 
  11. ↑ 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. 
  12. ↑ 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. 
  13. ↑ 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. 
  14. ↑ 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. 
  15. ↑ 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. 
  16. ↑ 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. 
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