The place of tachykinin NK2 receptor antagonists in the treatment diarrhea-predominant irritable bowel syndrome

A Szymaszkiewicz, A Malkiewicz… - … of Physiology and …, 2019 - publicum.umed.lodz.pl
Tachykinins act as neurotransmitters and neuromodulators in the central and peripheral
nervous system. Preclinical studies and clinical trials showed that inhibition of the tachykinin …

Targeting tachykinin receptors for the treatment of functional gastrointestinal disorders with a focus on irritable bowel syndrome

M Corsetti, F Akyuz, J Tack - Neurogastroenterology & Motility, 2015 - Wiley Online Library
Background Tachykinins (TK s) are a family of endogenous peptides widely expressed in
the central and in the peripheral nervous systems as well as in the gastrointestinal (GI) tract …

Randomised clinical trial: the clinical effects of a novel neurokinin receptor antagonist, DNK333, in women with diarrhoea‐predominant irritable bowel syndrome

S Zakko, G Barton, E Weber… - Alimentary …, 2011 - Wiley Online Library
Background Neurokinin receptors may play an important role in the visceral hypersensitivity
and exaggerated motor/secretory activity associated with diarrhoea‐predominant irritable …

The neurokinin-2 receptor antagonist ibodutant improves overall symptoms, abdominal pain and stool pattern in female patients in a phase II study of diarrhoea …

J Tack, K Schumacher, G Tonini, S Scartoni, A Capriati… - Gut, 2017 - gut.bmj.com
Background Tachykinins have been implicated in the pathophysiology of IBS with diarrhoea
(IBS-D). Our aim was to study the efficacy and safety of ibodutant, a selective neurokinin-2 …

Tachykinin receptor antagonists in irritable bowel syndrome.

A Lecci, C Valenti, CA Maggi - Current Opinion in Investigational …, 2002 - europepmc.org
Tachykinins (TKs) are abundantly expressed in the gastrointestinal (GI) tract in intrinsic
excitatory motor neurons, interneurons, sensory neurons and extrinsic sensory neurons …

Establishment and validation of a rabbit model for in vivo pharmacodynamic screening of tachykinin NK2 antagonists

T Tanaka, S Matsumoto-Okano, N Inatomi… - Journal of …, 2012 - Elsevier
We attempted to establish and validate an in vivo pharmacodynamic (PD) rabbit model to
screen tachykinin NK 2 receptor (NK 2-R) antagonists using pharmacological and …

Effects of tachykinin NK1 receptor antagonists on the viscerosensory response caused by colorectal distention in rabbits

S Okano, Y Ikeura, N Inatomi - Journal of Pharmacology and Experimental …, 2002 - ASPET
Irritable bowel syndrome (IBS) is a common disorder mainly characterized by altered bowel
habits and visceral pain. In this study, we investigated the role of tachykinin NK1 receptors in …

Tachykinins: role in human gastrointestinal tract physiology and pathology

G Improta, M Broccardo - Current Drug Targets, 2006 - ingentaconnect.com
Tachykinins (TKs) and their receptors (NK1, NK2 and NK3), which are diffusely expressed in
the human gastrointestinal tract, represent an endogenous modulator system regulating …

Tachykinin NK2 receptor antagonists for the treatment of irritable bowel syndrome

A Lecci, A Capriati, CA Maggi - British journal of pharmacology, 2004 - Wiley Online Library
Tachykinin NK2 receptors are expressed in the gastrointestinal tract of both laboratory
animals and humans. Experimental data indicate a role for these receptors in the regulation …

Multifaceted Approach to Determine the Antagonist Molecular Mechanism and Interaction of Ibodutant ([1-(2-Phenyl-1R-{[1-(tetrahydropyran-4-ylmethyl)-piperidin-4 …

S Meini, F Bellucci, C Catalani, P Cucchi… - … of Pharmacology and …, 2009 - ASPET
Ibodutant (MEN15596,[1-(2-phenyl-1 R-{[1-(tetrahydropyran-4-ylmethyl)-piperidin-4-
ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide) is a tachykinin NK2 receptor …