BIE-0246

BIIE-0246
BIE-0246
BIIE-0246 structure.png
임상 데이터
기타 이름BIE-0246
식별자
  • N-[(1S)-4-[(아미노미노메틸)아미노]-1-[(2-(3,5-다이옥소-1,2-디페닐-1,2,4-트리아졸리딘-4-일)에틸]아미노)카르보닐]부틸]-1-2(4-6-6-히드로)
CAS 번호
PubChem CID
IUPHAR/BPS
켐스파이더
유니
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C49H57N11O6
몰 질량896.066g/120−1
3D 모델(JSmol)
  • O=C3N(c1cc1)N(c2cc2)C(=O)N3CCNC(=O)[C@H](NC(=O)CC4(CCCC4)CC(=O)N8CCN(C7c5c(cc5)NC(=O)c6cc67)CC8)CC/N=C(\N)n
  • InChI=1S/C49H57N11O6/c50-46(51)53-25-13-22-40(45)52-26-27-58-47(65)59(34-14-3-4-15-34)60(4858)35-165-2-6-16541)
  • 키: RSJAXPUYVJKAAA-JPGJPTAESA-N ☒N
☒NcheckY (이게 뭐죠?) (표준)

BIE-0246은 Neuro펩타이드 [1]Y 수용체에2 대한 강력하고 선택적인 길항제 역할을 하는 과학 연구에 사용되는 약물이다.이는 최초로 개발된 비펩타이드 Y 선택성2 길항제 중 하나이며, 이 수용체를 연구하기 위해 가장 널리 사용되는 도구 중 하나이다.도파민 및 아세틸콜린 [5]방출을 조절하는[4] 것뿐만 아니라 추가적인 신경펩타이드 [2][3]Y 방출을 제한하는 시냅스 전 자가수용체로서의 Y 아형의2 역할을 입증하기 위해 사용되어 왔다.선택적[6][7]2 Y작용제가 항문제로 [9][10]유용할 것으로 예상되지만,[8] BIE-0246은 단독으로 [11]투여했을 때 식욕을 증가시키지 않는 것으로 나타났다.

레퍼런스

  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.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.
  7. ^ 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.
  8. ^ 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.
  9. ^ Félétou M, Levens NR (October 2005). "Neuropeptide Y2 receptors as drug targets for the central regulation of body weight". Current Opinion in Investigational Drugs. 6 (10): 1002–11. PMID 16259221.
  10. ^ 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.
  11. ^ 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.