BU08028

BU08028
BU08028
BU08028 structure.png
식별자
  • (1S2,81,62,1412,20, 2S, 6R, 14R, 16R)-5-(시클로프로필메틸)-16-[(2S)-2-히드록시-3, 3-디메틸펜탄-2-일]-15-메톡시-13-옥사-5-자헥사실로(132.02).
CAS 번호
PubChem CID
켐스파이더
화학 및 물리 데이터
공식C30H43NO4
몰 질량481.677 g/g−1/g
3D 모델(JSmol)
  • CCC(C)(C)[C@](C)([C@H]1)C[C@@]23CC[C@@]1([C@H]4)[C@@] 25CCN([C@@H]3)CC6=C5C(=C(C=C6)O)O4) CC7CC7)OC)O
  • InChI=1S/C30H43NO4/c1-6-26(2,3)27(4,33)21-16-28-11-30(21,34-5)25-29(28)13-31(17-18-8-18)22(28)15-19-9-10-24-32)
  • 키: HBENZIXOGRCSQN-VQWACLZSA-N

BU08028은 μ-오피오이드 수용체와 노시셉틴 수용체 모두에서 강력한 부분작용제 역할을 하는 약물이다.그것은 측쇄에 탄소 1개만 연장된 부프레놀핀의 상동체이지만, 노키셉틴 수용체에서 상대적으로 더 큰 활성을 가지며,[1][2][3][4] 진통제를 손상시키지 않고 남용 가능성을 감소시키는 것으로 생각된다.

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레퍼런스

  1. ^ Cami-Kobeci G, Polgar WE, Khroyan TV, Toll L, Husbands SM (October 2011). "Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine". Journal of Medicinal Chemistry. 54 (19): 6531–7. doi:10.1021/jm2003238. PMC 3188691. PMID 21866885.
  2. ^ Khroyan TV, Polgar WE, Cami-Kobeci G, Husbands SM, Zaveri NT, Toll L (March 2011). "The first universal opioid ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): characterization of the in vitro profile and in vivo behavioral effects in mouse models of acute pain and cocaine-induced reward". The Journal of Pharmacology and Experimental Therapeutics. 336 (3): 952–61. doi:10.1124/jpet.110.175620. PMC 3061529. PMID 21177476.
  3. ^ Ding H, Czoty PW, Kiguchi N, Cami-Kobeci G, Sukhtankar DD, Nader MA, et al. (September 2016). "A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates". Proceedings of the National Academy of Sciences of the United States of America. 113 (37): E5511-8. doi:10.1073/pnas.1605295113. PMC 5027459. PMID 27573832.
  4. ^ Kiguchi N, Ding H, Ko MC (April 2020). "Therapeutic potentials of NOP and MOP receptor coactivation for the treatment of pain and opioid abuse". Journal of Neuroscience Research. doi:10.1002/jnr.24624. PMC 7573817. PMID 32255240.
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