Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials. (Q39456171)

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English	Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials.	scientific article

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scholarly article

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12 February 2020

Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials (English)

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12 February 2020

phase I clinical trial

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pharmacokinetics

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inferred from title

pharmacodynamics

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1

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12 February 2020

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Wolfram Nothaft

2

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12 February 2020

Walid M Awni

3

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12 February 2020

Sandeep Dutta

4

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publication date

1 April 2013

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12 February 2020

British Journal of Clinical Pharmacology

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12 February 2020

75

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12 February 2020

1029-1040

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12 February 2020

4

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12 February 2020

An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UV(B)-inflamed and normal skin

1 reference

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Transient receptor potential channels as therapeutic targets

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An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects

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12 September 2017

Pharmacokinetics of the TRPV1 antagonist ABT-102 in healthy human volunteers: population analysis of data from 3 phase 1 trials

1 reference

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Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway

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(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

1 reference

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12 September 2017

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

1 reference

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Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade

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Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors

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The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation

1 reference

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Lipopolysaccharide fever is initiated via a capsaicin-sensitive mechanism independent of the subtype-1 vanilloid receptor

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Thermosensation and pain

1 reference

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Vanilloid receptors take a TRP beyond the sensory afferent☆

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The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1)

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The capsaicin receptor: a heat-activated ion channel in the pain pathway

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12 September 2017

Population Pharmacokinetics/Dynamics*

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12 September 2017

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

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14 September 2017

Cold-seeking behavior as a thermoregulatory strategy in systemic inflammation.

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Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist

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Capsaicin and central control of thermoregulation

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21 August 2018

Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial

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21 August 2018

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

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Identifiers

10.1111/J.1365-2125.2012.04405.X

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24 November 2022

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12 February 2020

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