BIIE-0246

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
Identifikatori
CAS broj	246146-55-4
PubChem	CID 5311024
IUPHAR/BPS	1547
Sinonimi	BIIE-0246
Hemijski podaci
Formula	C49H57N11O6
Molarna masa	896.045 g/mol
	SMILES c8ccccc8-n(c3=O)n(-c6ccccc6)c(=O)n3CCNC(=O)C(CCCNC(=N)N)NC(=O)CC4(CCCC4)CC(=O)N5CCN(CC5)C(c7ccccc27)c1ccccc1NC2=O; ;

BIIE-0246 je lek koji se koristi u naučnim istraživanjima, i koji deluje kao potentan i selektivan antagonist neuropepdnog Y receptora Y₂.^[1] 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,^[2]^[3] kao i da modulira oslobađanje dopamina^[4] i acetilholina.^[5] Bilo je pokazano da utiče na ponašanje životinja. Ovaj materijal umanjuje alkoholni utrošak kod zavisnih pacova^[6]^[7] kao i anksiolitičke efekte.^[8] Dok bi selektivni Y₂ agonisti trebalo da budu korisni kao anoreksici,^[9]^[10] BIIE-0246 nema uticaja na apetit.^[11]

Reference

^ Doods H, Gaida W, Wieland HA, Dollinger H, Schnorrenberg G, Esser F, Engel W, Eberlein W, Rudolf K (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.
^ King PJ, Williams G, Doods H, Widdowson PS (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.
^ Malmström RE, Lundberg JO, Weitzberg E (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.
^ Adewale AS, Macarthur H, Westfall TC (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.
^ Herring N, Lokale MN, Danson EJ, Heaton DA, Paterson DJ (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.
^ Thorsell A, Rimondini R, Heilig M (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.
^ Rimondini R, Thorsell A, Heilig M (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.
^ Bacchi F, Mathé AA, Jiménez P, Stasi L, Arban R, Gerrard P, Caberlotto L (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.
^ Félétou M, Levens NR (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.
^ Parker SL, Balasubramaniam A (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.
^ Scott V, Kimura N, Stark JA, Luckman SM (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.

Spoljašnje veze

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[pmid10611450-1] Doods H, Gaida W, Wieland HA, Dollinger H, Schnorrenberg G, Esser F, Engel W, Eberlein W, Rudolf K (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.

[pmid10822055-2] King PJ, Williams G, Doods H, Widdowson PS (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.

[pmid11937100-3] Malmström RE, Lundberg JO, Weitzberg E (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.

[pmid17382974-4] Adewale AS, Macarthur H, Westfall TC (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.

[pmid17996892-5] Herring N, Lokale MN, Danson EJ, Heaton DA, Paterson DJ (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.

[pmid12377370-6] Thorsell A, Rimondini R, Heilig M (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.

[pmid15670655-7] Rimondini R, Thorsell A, Heilig M (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.

[pmid16959374-8] Bacchi F, Mathé AA, Jiménez P, Stasi L, Arban R, Gerrard P, Caberlotto L (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.

[pmid16259221-9] Félétou M, Levens NR (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.

[pmid17828288-10] Parker SL, Balasubramaniam A (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.

[pmid15946163-11] Scott V, Kimura N, Stark JA, Luckman SM (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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