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
Klinički podaci
Identifikatori
CAS broj	246146-55-4
ATC kod	?
PubChem	5311024
Hemijski podaci
Formula	C49H57N11O6
Mol. masa	896.045 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C49H57N11O6/c50-46(51)53-25-13-22-40(45(64)52-26-27-58-47(65)59(34-14-3-1-4-15-34)60(48(58)66)35-16-5-2-6-17-35)54-41(61)32-49(23-11-12-24-49)33-42(62)56-28-30-57(31-29-56)43-36-18-7-8-19-37(36)44(63)55-39-21-10-9-20-38(39)43/h1-10,14-21,40,43H,11-13,22-33H2,(H,52,64)(H,54,61)(H,55,63)(H4,50,51,53)/t40-,43?/m0/s1 ; Key: RSJAXPUYVJKAAA-JPGJPTAESA-N
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

↑ 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
↑ 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.
↑ 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. DOI:10.1016/S0014-2999(99)00650-0. PMID 10611450.
↑ 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. DOI:10.1016/S0014-2999(00)00230-2. PMID 10822055.
↑ 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. DOI:10.1016/S0014-2999(02)01371-7. PMID 11937100.
↑ 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. DOI:10.1016/j.neuropharm.2007.01.018. PMID 17382974.
↑ 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. DOI:10.1016/j.yjmcc.2007.10.001. PMID 17996892.
↑ 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. DOI:10.1016/S0304-3940(02)00904-7. PMID 12377370.
↑ 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. DOI:10.1016/j.neulet.2004.10.084. PMID 15670655.
↑ 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. DOI:10.1016/j.peptides.2006.07.020. PMID 16959374.
↑ 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.
↑ Parker SL, Balasubramaniam A (February 2008). „Neuropeptide Y Y2 receptor in health and disease”. British Journal of Pharmacology 153 (3): 420–31. DOI:10.1038/sj.bjp.0707445. PMC 2241788. PMID 17828288.
↑ 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. DOI:10.1111/j.1365-2826.2005.01330.x. PMID 15946163.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Šablon:Neuropeptidni ligandi

[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.

[pmid10611450-3] 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. DOI:10.1016/S0014-2999(99)00650-0. PMID 10611450.

[pmid10822055-4] 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. DOI:10.1016/S0014-2999(00)00230-2. PMID 10822055.

[pmid11937100-5] 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. DOI:10.1016/S0014-2999(02)01371-7. PMID 11937100.

[pmid17382974-6] 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. DOI:10.1016/j.neuropharm.2007.01.018. PMID 17382974.

[pmid17996892-7] 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. DOI:10.1016/j.yjmcc.2007.10.001. PMID 17996892.

[pmid12377370-8] 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. DOI:10.1016/S0304-3940(02)00904-7. PMID 12377370.

[pmid15670655-9] 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. DOI:10.1016/j.neulet.2004.10.084. PMID 15670655.

[pmid16959374-10] 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. DOI:10.1016/j.peptides.2006.07.020. PMID 16959374.

[pmid16259221-11] 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.

[pmid17828288-12] Parker SL, Balasubramaniam A (February 2008). „Neuropeptide Y Y2 receptor in health and disease”. British Journal of Pharmacology 153 (3): 420–31. DOI:10.1038/sj.bjp.0707445. PMC 2241788. PMID 17828288.

[pmid15946163-13] 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. DOI:10.1111/j.1365-2826.2005.01330.x. PMID 15946163.

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