Tetrahydroquinoline derivatives as opioid receptor antagonists

被引：8

作者：

Zhang, Cunyu ^{[1
]}

Westaway, Susan M. ^{[2
]}

Speake, Jason D. ^{[1
]}

Bishop, Michael J. ^{[1
]}

Goetz, Aaron S. ^{[3
]}

Carballo, Luz Helena ^{[3
]}

Hu, Mike ^{[4
]}

Epperly, Andrea H. ^{[4
]}

机构：

[1] GlaxoSmithKline, Dept Med Chem, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline, Immunoinflammat CEDD, Stevenage SG1 2NY, Herts, England

[3] GlaxoSmithKline, Mol Discovery Res, Screening & Compound Profiling, Res Triangle Pk, NC 27709 USA

[4] GlaxoSmithKline, Dept Drug Metab & Pharmacokinet, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 02期

关键词：

Tetrahydroquinoline; Opioid; Antagonist; NALOXONE; ANALOGS; RATS; FOOD;

D O I：

10.1016/j.bmcl.2010.12.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58 nM (K-i) functional activity against the mu opioid receptor. DMPK data suggest that novel tetrahydroquinoline analogs may be advantageous in peripheral applications. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：670 / 676

页数：7

共 50 条

[21] DERIVATIVES OF TETRAHYDROQUINOLINE AND TETRAHYDROISOQUINOLINE
BAHNER, CT
EASLEY, WK
STEPHEN, E
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1952, 74 (16) : 4198 - 4199
[22] Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists
Gong, Yong
Barbay, J. Kent
Buntinx, Mieke
Li, Jian
Van Wauweb, Jean
Claes, Concha
Van Lommen, Guy
Hornby, Pamela J.
He, Wei
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (14) : 3852 - 3855
[23] Aminoguanidine Hydrazone Derivatives as Nonpeptide NPFF1 Receptor Antagonists Reverse Opioid Induced Hyperalgesia
Hammoud, Hassan
Elhabazi, Khadija
Quillet, Raphaelle
Bertin, Isabelle
Utard, Valerie
Laboureyras, Emilie
Bourguignon, Jean-Jacques
Bihel, Frederic
Simonnet, Guy
Simonin, Frederic
Schmitt, Martine
ACS CHEMICAL NEUROSCIENCE, 2018, 9 (11): : 2599 - 2609
[24] Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands
Harland, Aubrie A.
Bender, Aaron M.
Griggs, Nicholas W.
Gao, Chao
Anand, Jessica P.
Pogozheya, Irma D.
Traynor, John R.
Jutkiewicz, Emily M.
Mosberg, Henry I.
JOURNAL OF MEDICINAL CHEMISTRY, 2016, 59 (10) : 4985 - 4998
[25] XANTHINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS
FREDHOLM, BB
PERSSON, CGA
EUROPEAN JOURNAL OF PHARMACOLOGY, 1982, 81 (04) : 673 - 676
[26] The Importance of Micelle-Bound States for the Bioactivities of Bifunctional Peptide Derivatives for δ/μ Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists
Yamamoto, Takashi
Nair, Padma
Jacobsen, Neil E.
Davis, Peg
Ma, Shou-wu
Navratilova, Edita
Moye, Sharif
Lai, Josephine
Yamamura, Henry I.
Vanderah, Todd W.
Porreca, Frank
Hruby, Victor J.
JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (20) : 6334 - 6347
[27] OPIOID RECEPTOR AFFINITIES OF KAPPA AGONISTS, AGONIST ANTAGONISTS AND ANTAGONISTS INVITRO AND INVIVO
WOOD, PL
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY, 1983, 7 (4-6): : 657 - 662
[28] Recent advances in selective opioid receptor agonists and antagonists
Eguchi, M
MEDICINAL RESEARCH REVIEWS, 2004, 24 (02) : 182 - 212
[29] Antipruritic treatment with systemic μ-opioid receptor antagonists: A review
Phan, Ngoc Quan
Bernhard, Jeffrey D.
Luger, Thomas A.
Staender, Sonja
JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, 2010, 63 (04) : 680 - 688
[30] PRECIPITATED WITHDRAWAL FROM BUTORPHANOL BY OPIOID RECEPTOR ANTAGONISTS
JAW, SP
MAKIMURA, M
OH, KW
HOSKINS, B
HO, IK
FASEB JOURNAL, 1991, 5 (04): : A497 - A497

← 1 2 3 4 5 →