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Last update 23 Jan 2025

NK2R

Last update 23 Jan 2025

Basic Info

Synonyms

Neurokinin 2, Neurokinin A receptor, neurokinin B receptor

+ [10]

Introduction

This is a receptor for the tachykinin neuropeptide substance K (neurokinin A). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance K > neuromedin-K > substance P.

Drugs associated with NK2R

FK-224

Target

NK1R x NK2R

Mechanism

NK1R antagonists [+1]

Active Org.

Fujisawa Pharmaceutical Co., Ltd.

Originator Org.

Astellas Pharma, Inc.

Active Indication-

Inactive Indication

Angina Pectoris [+2]

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

YM-44781

Target

NK2R

Mechanism

NK2R antagonists

Active Org.

Roche Holding AG

Originator Org.

Roche Holding AG

Active Indication

Contracted bladder

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

TAK-480

Target

NK2R

Mechanism

NK2R antagonists

Active Org.

Takeda Pharmaceuticals LLC

Originator Org.

Takeda Pharmaceuticals LLC

Active Indication

Irritable Bowel Syndrome

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with NK2R

NCT02320318

/ WithdrawnPhase 3

A 12-week Double-blind, Randomised, Placebo-controlled, Parallel Group Phase III Study, Followed by a 4-week Randomised Withdrawal Period to Evaluate the Efficacy and Safety of Oral Ibodutant 10 mg Once Daily in Female Patients With Irritable Bowel Syndrome With Diarrhoea (IBS-D).

Irritable Bowel Syndrome with diarrhoea (IBS-D) is a functional gastrointestinal disorder characterised by chronic or recurrent abdominal pain or discomfort and diarrhoea. The aim of this trial is the evaluation of the efficacy and safety of oral ibodutant 10 mg once daily as compared to placebo in women with IBS-D over a 12-week treatment period.

Start Date01 Oct 2015

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite SRL

NCT02107196

/ CompletedPhase 3

A 12-Week Double-blind, Randomised, Placebo-controlled, Parallel Group Phase III Study, Followed by a 4-Week Randomised Withdrawal Period to Evaluate the Efficacy and Safety of Oral Ibodutant 10 mg Once Daily in Female Patients With Irritable Bowel Syndrome With Diarrhea

Irritable Bowel Syndrome with diarrhoea (IBS-D) is a functional gastrointestinal disorder characterised by chronic or recurrent abdominal pain or discomfort and diarrhoea. This trial aims at the evaluation of the efficacy and safety of oral ibodutant 10 mg once daily as compared to placebo in women with IBS-D over a 12-week treatment period.

Start Date01 Mar 2014

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite SRL

NCT02120027

/ TerminatedPhase 3

A 52-Week, Double-blind, Randomised, Placebo-controlled, Parallel-group Phase III Study With Re-randomisations at Week 25 to Evaluate the Efficacy and Safety of Oral Ibodutant 10 mg Once Daily in Female Patients With Irritable Bowel Syndrome With Diarrhoea (IBS-D)

Irritable Bowel Syndrome with diarrhoea (IBS-D) is a functional gastrointestinal disorder characterised by chronic or recurrent abdominal pain or discomfort and diarrhoea. This trial aims at the evaluation of the efficacy and safety of oral ibodutant 10 mg once daily as compared to placebo in women with IBS-D over a 24-week treatment period.

Start Date01 Feb 2014

Sponsor / Collaborator

A. Menarini Industrie Farmaceutiche Riunite SRL

100 Clinical Results associated with NK2R

100 Translational Medicine associated with NK2R

0 Patents (Medical) associated with NK2R

628

Literatures (Medical) associated with NK2R

01 Jan 2025·Nature Reviews Drug Discovery

NK2R agonist delivers one-two punch to obesity

Communications

Author: Crunkhorn, Sarah

01 Jan 2025·Scandinavian Journal of Immunology

Substance P and neurokinin 1 receptor boost the pathogenicity of granulocyte‐macrophage colony‐stimulating factor‐producing T helper cells in dry eye disease

Article

Author: Liu, Qingqing ; Zhang, Hui ; Rong, Hua ; Wang, Shaolin ; Yang, Hai

AbstractDry eye disease (DED) is an inflammatory disorder in which CD4+ T cells play a significant role in its pathogenesis. A CD4+ T cell subset termed granulocyte‐macrophage colony‐stimulating factor‐producing T helper (ThGM) cells would contribute to DED pathogenesis. However, the mechanisms by which the activity of ThGM cells is modulated are not thoroughly understood. In this research, we characterized the effects of neurokinin 1 receptor (NK1R) and neurokinin 2 receptor (NK2R) on ThGM cells and T helper 1 (Th1) cells in a murine DED model. We found that ThGM cells expressed NK1R and NK2R, whereas Th1 cells predominantly expressed NK1R. Furthermore, substance P and neurokinin A (NKA), the ligands of NK1R and NK2R, were upregulated in post‐DED LNs and conjunctivae. Substance P significantly promoted granulocyte‐macrophage colony‐stimulating factor (GM‐CSF) expression while mildly upregulating the expression of interferon‐gamma (IFN‐γ) and interleukin 2 (IL‐2) in ThGM cells. By contrast, NKA did not change GM‐CSF expression but significantly increased IFN‐γ expression in ThGM cells. Importantly, the adoptive transfer of NK1R‐expressing ThGM cells significantly exacerbated DED, whereas the transfer of NK1R‐knockdown ThGM cells weakly aggravated DED. NK2R knockdown in ThGM cells did not affect DED progression. In conclusion, this study identifies the substance P‐NK1R axis as a novel mechanism that reinforces the pathogenicity of ThGM cells in DED.

01 Dec 2024·Annals of Internal Medicine

How Would You Manage This Patient With Gastroesophageal Reflux Symptoms? Grand Rounds Discussion From Beth Israel Deaconess Medical Center

Article

Author: Libman, Howard ; Anderson, Timothy S. ; Reynolds, Eileen E. ; Rangan, Vikram V.

Gastroesophageal reflux disease (GERD) is a common medical condition presenting with heartburn, regurgitation, cough, hoarseness, and/or wheezing. Patients with classic GERD symptoms often do not require diagnostic studies before empirical treatment is initiated. However, if atypical features are present, including alarm symptoms for malignancy, or if symptoms do not respond to conventional treatment, upper endoscopy may be necessary. The optimal management of GERD, which is the subject of debate, depends on the frequency and severity of symptoms. In 2021, the American College of Gastroenterology published updated recommendations for diagnosis and management of GERD. In addition to histamine-2 receptor antagonist or proton-pump inhibitor therapy, which may be prescribed as needed or continuously, lifestyle and dietary modification are often advised. Here, 2 physicians, a primary care practitioner and a gastroenterologist, debate how to manage a patient with GERD symptoms. They discuss the diagnosis of this condition, its initial management, indications for upper endoscopy, and how to care for the patient whose condition does not respond to empirical therapy.

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NK2R

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