Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists. (Q45939059)

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English	Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists.	scientific article

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scholarly article

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Europe PubMed Central

PubMed publication ID

18 December 2017

http://europepmc.org/abstract/MED/24884675

Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists. (English)

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Europe PubMed Central

PubMed publication ID

18 December 2017

http://europepmc.org/abstract/MED/24884675

object named as

Ryan West

7

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Ardem Patapoutian

12

object named as

Ardem Patapoutian

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Europe PubMed Central

PubMed publication ID

18 December 2017

http://europepmc.org/abstract/MED/24884675

11

object named as

Matt J Petrus

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Europe PubMed Central

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18 December 2017

http://europepmc.org/abstract/MED/24884675

author name string

Lisa Rooney

1

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Agnès Vidal

2

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Anne-Marie D'Souza

3

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Nick Devereux

4

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Brian Masick

5

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Valerie Boissel

6

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Victoria Head

8

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Rowan Stringer

9

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Jianmin Lao

10

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Mark Nash

13

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Natalie Stoakley

14

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Moh Panesar

15

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18 December 2017

http://europepmc.org/abstract/MED/24884675

J Martin Verkuyl

16

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Andrew M Schumacher

17

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18 December 2017

http://europepmc.org/abstract/MED/24884675

H Michael Petrassi

18

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18 December 2017

http://europepmc.org/abstract/MED/24884675

David C Tully

19

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18 December 2017

http://europepmc.org/abstract/MED/24884675

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publication date

13 June 2014

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Journal of Medicinal Chemistry

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18 December 2017

http://europepmc.org/abstract/MED/24884675

57

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18 December 2017

http://europepmc.org/abstract/MED/24884675

12

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18 December 2017

http://europepmc.org/abstract/MED/24884675

5129-5140

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Europe PubMed Central

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18 December 2017

http://europepmc.org/abstract/MED/24884675

Targeting TRP channels for pain relief

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2-Amino-4-arylthiazole compounds as TRPA1 antagonists (WO 2012085662): a patent evaluation

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Models and mechanisms of hyperalgesia and allodynia

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A novel role for AMP-kinase in the regulation of the Na+/I--symporter and iodide uptake in the rat thyroid gland.

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The nociceptor ion channel TRPA1 is potentiated and inactivated by permeating calcium ions.

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Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans

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Suzuki-Miyaura cross-coupling of unprotected, nitrogen-rich heterocycles: substrate scope and mechanistic investigation

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Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents

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Species-specific pharmacology of Trichloro(sulfanyl)ethyl benzamides as transient receptor potential ankyrin 1 (TRPA1) antagonists

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A modern in vivo pharmacokinetic paradigm: combining snapshot, rapid and full PK approaches to optimize and expedite early drug discovery

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7-tert-Butyl-6-(4-chloro-phenyl)-2-thioxo-2,3-dihydro-1H-pyrido[2,3-d]pyrimidin-4-one, a classic polymodal inhibitor of transient receptor potential vanilloid type 1 with a reduced liability for hyperthermia, is analgesic and ameliorates visceral hy

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TRPA1 contributes to cold, mechanical, and chemical nociception but is not essential for hair-cell transduction

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Caffeine activates mouse TRPA1 channels but suppresses human TRPA1 channels

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Transient receptor potential A1 is a sensory receptor for multiple products of oxidative stress

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TRPA1 receptor induced relaxation of the human urethra involves TRPV1 and cannabinoid receptor mediated signals, and cyclooxygenase activation

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TRPA1 receptors mediate environmental irritant-induced meningeal vasodilatation

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TRPA1 mediates the inflammatory actions of environmental irritants and proalgesic agents

1 reference

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4-Hydroxynonenal, an endogenous aldehyde, causes pain and neurogenic inflammation through activation of the irritant receptor TRPA1

1 reference

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Relative contributions of TRPA1 and TRPV1 channels in the activation of vagal bronchopulmonary C-fibres by the endogenous autacoid 4-oxononenal

1 reference

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TRPA1 regulates gastrointestinal motility through serotonin release from enterochromaffin cells

1 reference

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Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines

1 reference

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The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain.

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Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals

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A gain-of-function mutation in TRPA1 causes familial episodic pain syndrome

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ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures

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Transient receptor potential channels - emerging novel drug targets for the treatment of pain

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TRPA1 and Substance P Mediate Colitis in Mice

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The analgesic effects of R(+)-WIN 55,212-2 mesylate, a high affinity cannabinoid agonist, in a rat model of neuropathic pain

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Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation

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TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats

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Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel.

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Differential expression profile of cold (TRPA1) and cool (TRPM8) receptors in human urogenital organs

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A new model of visceral pain and referred hyperalgesia in the mouse

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Transient receptor potential channel A1 is directly gated by calcium ions

1 reference

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A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition.

1 reference

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Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1

1 reference

12 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1021/JM401986P

Identifiers

10.1021/JM401986P

1 reference

Europe PubMed Central

PubMed publication ID

18 December 2017

http://europepmc.org/abstract/MED/24884675

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

18 December 2017

http://europepmc.org/abstract/MED/24884675

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