BIIE-0246

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BIIE-0246
(IUPAC) ime
N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[([2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino)carbonyl]butyl]-1-(2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]-2-oxoethyl)cyclopentaneacetamide
Klinički podaci
Identifikatori
CAS broj 246146-55-4
ATC kod ?
PubChem[1][2] 5311024
Hemijski podaci
Formula C49H57N11O6 
Mol. masa 896.045 g/mol
SMILES eMolekuli & PubHem
Sinonimi BIIE-0246
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

BIIE-0246 je lek koji se koristi u naučnim istraživanjima, i koji deluje kao potentan i selektivan antagonist neuropepdnog Y receptora Y2.[3] On je bio jedan od prvih ne-peptidnih Y2-selektivnih antagonista, i još uvek je jedno od najšire korišćenih oruđa za izučavanje tog receptora. Pomoću njega je demonstrirano da Y2 ima ulogu presinaptičkog autoreceptora koji ograničava dalje oslobađanje neuropeptida Y,[4][5] kao i da modulira oslobađanje dopamina[6] i acetilholina.[7] Bilo je pokazano da utiče na ponašanje životinja. Ovaj materijal umanjuje alkoholni utrošak kod zavisnih pacova[8][9] kao i anksiolitičke efekte.[10] Dok bi selektivni Y2 agonisti trebalo da budu korisni kao anoreksici,[11][12] BIIE-0246 nema uticaja na apetit.[13]

Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. ↑ Doods H, Gaida W, Wieland HA, Dollinger H, Schnorrenberg G, Esser F, Engel W, Eberlein W, Rudolf K (November 1999). "BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist". European Journal of Pharmacology 384 (2-3): R3–5. PMID 10611450. doi:10.1016/S0014-2999(99)00650-0. 
  4. ↑ King PJ, Williams G, Doods H, Widdowson PS (May 2000). "Effect of a selective neuropeptide Y Y(2) receptor antagonist, BIIE0246 on neuropeptide Y release". European Journal of Pharmacology 396 (1): R1–3. PMID 10822055. doi:10.1016/S0014-2999(00)00230-2. 
  5. ↑ Malmström RE, Lundberg JO, Weitzberg E (March 2002). "Autoinhibitory function of the sympathetic prejunctional neuropeptide Y Y(2) receptor evidenced by BIIE0246". European Journal of Pharmacology 439 (1-3): 113–9. PMID 11937100. doi:10.1016/S0014-2999(02)01371-7. 
  6. ↑ Adewale AS, Macarthur H, Westfall TC (May 2007). "Neuropeptide Y-induced enhancement of the evoked release of newly synthesized dopamine in rat striatum: mediation by Y2 receptors". Neuropharmacology 52 (6): 1396–402. PMID 17382974. doi:10.1016/j.neuropharm.2007.01.018. 
  7. ↑ Herring N, Lokale MN, Danson EJ, Heaton DA, Paterson DJ (March 2008). "Neuropeptide Y reduces acetylcholine release and vagal bradycardia via a Y2 receptor-mediated, protein kinase C-dependent pathway". Journal of Molecular and Cellular Cardiology 44 (3): 477–85. PMID 17996892. doi:10.1016/j.yjmcc.2007.10.001. 
  8. ↑ Thorsell A, Rimondini R, Heilig M (October 2002). "Blockade of central neuropeptide Y (NPY) Y2 receptors reduces ethanol self-administration in rats". Neuroscience Letters 332 (1): 1–4. PMID 12377370. doi:10.1016/S0304-3940(02)00904-7. 
  9. ↑ Rimondini R, Thorsell A, Heilig M (February 2005). "Suppression of ethanol self-administration by the neuropeptide Y (NPY) Y2 receptor antagonist BIIE0246: evidence for sensitization in rats with a history of dependence". Neuroscience Letters 375 (2): 129–33. PMID 15670655. doi:10.1016/j.neulet.2004.10.084. 
  10. ↑ Bacchi F, Mathé AA, Jiménez P, Stasi L, Arban R, Gerrard P, Caberlotto L (December 2006). "Anxiolytic-like effect of the selective neuropeptide Y Y2 receptor antagonist BIIE0246 in the elevated plus-maze". Peptides 27 (12): 3202–7. PMID 16959374. doi:10.1016/j.peptides.2006.07.020. 
  11. ↑ Félétou M, Levens NR (October 2005). "Neuropeptide Y2 receptors as drug targets for the central regulation of body weight". Current Opinion in Investigational Drugs (London, England : 2000) 6 (10): 1002–11. PMID 16259221. 
  12. ↑ Parker SL, Balasubramaniam A (February 2008). "Neuropeptide Y Y2 receptor in health and disease". British Journal of Pharmacology 153 (3): 420–31. PMC 2241788. PMID 17828288. doi:10.1038/sj.bjp.0707445. 
  13. ↑ Scott V, Kimura N, Stark JA, Luckman SM (July 2005). "Intravenous peptide YY3-36 and Y2 receptor antagonism in the rat: effects on feeding behaviour". Journal of Neuroendocrinology 17 (7): 452–7. PMID 15946163. doi:10.1111/j.1365-2826.2005.01330.x. 

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