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TRPV1 拮抗剂 ABT-116 的发现。

Discovery of TRPV1 antagonist ABT-116.

机构信息

Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Dept R4PM, AP10-207, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA.

出版信息

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3291-4. doi: 10.1016/j.bmcl.2010.04.047. Epub 2010 Apr 14.

DOI:10.1016/j.bmcl.2010.04.047
PMID:20457518
Abstract

The synthesis and SAR of a series of indazole TRPV1 antagonists leading to the discovery of 21 (ABT-116) is described. Biological studies demonstrated potent in vitro and in vivo activity for 21, as well as suitable physicochemical and pharmacokinetic properties for advancement to clinical development for pain management.

摘要

描述了一系列吲唑 TRPV1 拮抗剂的合成和 SAR 研究，导致了 21（ABT-116）的发现。生物学研究表明 21 具有很强的体外和体内活性，以及适合用于疼痛管理的临床开发的适当理化性质和药代动力学特性。

相似文献

[1]
Discovery of TRPV1 antagonist ABT-116.

Bioorg Med Chem Lett. 2010-4-14

[2]
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.

J Med Chem. 2007-7-26

[3]
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.

J Med Chem. 2008-2-14

[4]
Analgesic potential of TRPV1 antagonists.

Biochem Pharmacol. 2009-8-1

[5]
(R)-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) blocks polymodal activation of transient receptor potential vanilloid 1 receptors in vitro and heat-evoked firing of spinal dorsal horn neurons in vivo.

J Pharmacol Exp Ther. 2008-9

[6]
Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia.

Pain. 2009-3

[7]
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.

Bioorg Med Chem Lett. 2007-7-15

[8]
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.

J Med Chem. 2007-7-26

[9]
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.

Bioorg Med Chem Lett. 2006-10-1

[10]
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.

J Med Chem. 2010-4-22

引用本文的文献

[1]
Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.

Curr Top Med Chem. 2025-1-2

[2]
Research trends and frontier hotspots of TRPV1 based on bibliometric and visualization analyses.

Heliyon. 2024-1-5

[3]
TRPV1-Targeted Drugs in Development for Human Pain Conditions.

Drugs. 2021-1

[4]
Novel scaffolds for modulation of TRPV1 identified with pharmacophore modeling and virtual screening.

Future Med Chem. 2015

[5]
3-substituted indazoles as configurationally locked 4EGI-1 mimetics and inhibitors of the eIF4E/eIF4G interaction.

Chembiochem. 2014-3-3

[6]
How Far Could We Go with Open Data - A Case Study for TRPV1 Antagonists.

Mol Inform. 2013-6

[7]
Effect of analgesic therapy on clinical outcome measures in a randomized controlled trial using client-owned dogs with hip osteoarthritis.

BMC Vet Res. 2012-10-4

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