Skip Content
You are currently on the new version of our website. Access the old version .

20 Results Found

  • Article
  • Open Access
19 Citations
4,915 Views
18 Pages

Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors

  • Paweł K. Halik,
  • Piotr F. J. Lipiński,
  • Joanna Matalińska,
  • Przemysław Koźmiński,
  • Aleksandra Misicka and
  • Ewa Gniazdowska

18 August 2020

Aprepitant, a lipophilic and small molecular representative of neurokinin 1 receptor antagonists, is known for its anti-proliferative activity on numerous cancer cell lines that are sensitive to Substance P mitogen action. In the presented research,...

  • Article
  • Open Access
9 Citations
9,457 Views
14 Pages

The Inhibitory Effect of Botulinum Toxin Type A on Rat Pyloric Smooth Muscle Contractile Response to Substance P In Vitro

  • Yu-Feng Shao,
  • Jun-Fan Xie,
  • Yin-Xiang Ren,
  • Can Wang,
  • Xiang-Pan Kong,
  • Xiao-Jian Zong,
  • Lin-Lan Fan and
  • Yi-Ping Hou

15 October 2015

A decrease in pyloric myoelectrical activity and pyloric substance P (SP) content following intrasphincteric injection of botulinum toxin type A (BTX-A) in free move rats have been demonstrated in our previous studies. The aim of the present study wa...

  • Review
  • Open Access
39 Citations
8,159 Views
28 Pages

The Significance of NK1 Receptor Ligands and Their Application in Targeted Radionuclide Tumour Therapy

  • Agnieszka Majkowska-Pilip,
  • Paweł Krzysztof Halik and
  • Ewa Gniazdowska

To date, our understanding of the Substance P (SP) and neurokinin 1 receptor (NK1R) system shows intricate relations between human physiology and disease occurrence or progression. Within the oncological field, overexpression of NK1R and this SP/NK1R...

  • Article
  • Open Access
1,550 Views
10 Pages

1 February 2024

Background: Prior speculation suggests that selective 5-hydroxytryptamine-3 receptors and neurokinin-1 receptor antagonists may increase arrhythmia risk and induce electrocardiographic changes. This study examined the effect of anti-emetic medication...

  • Article
  • Open Access
9 Citations
2,807 Views
16 Pages

In Vitro Biological Evaluation of Aprepitant Based 177Lu-Radioconjugates

  • Paweł K. Halik,
  • Przemysław Koźmiński,
  • Joanna Matalińska,
  • Piotr F. J. Lipiński,
  • Aleksandra Misicka and
  • Ewa Gniazdowska

Currently, the search for promising NK1R-positive tumor-targeting radiopharmaceuticals based on the structure of small molecular antagonists of neurokinin-1 receptor can be observed. Following this trend, we continued our evaluation of aprepitant-bas...

  • Feature Paper
  • Review
  • Open Access
6 Citations
7,018 Views
12 Pages

A New Hope for Woman with Vasomotor Symptoms: Neurokinin B Antagonists

  • Blazej Meczekalski,
  • Anna Kostrzak,
  • Christian Unogu,
  • Stefania Bochynska,
  • Marzena Maciejewska-Jeske,
  • Gregory Bala and
  • Anna Szeliga

21 February 2025

KNDy (kisspeptine, neurokinin B, dynorphin) neurons, located in the hypothalamus, play a crucial role in the development of vasomotor symptoms (VSM) in menopausal women. Estrogen withdrawal during menopause leads to the hyperactivation of kisspeptin...

  • Review
  • Open Access
79 Citations
13,606 Views
22 Pages

20 September 2020

Neurokinin-1 receptor (NK-1R) antagonists exert antitumor action, are safe and do not cause serious side-effects. These antagonists (via the NK-1R) exert multiple actions against cancer: antiproliferative and anti-Warburg effects and apoptotic, anti-...

  • Entry
  • Open Access
2 Citations
2,207 Views
10 Pages

Antitumor Strategies Targeting Peptidergic Systems

  • Francisco D. Rodríguez and
  • Rafael Coveñas

Peptidergic systems show promise as targets for fighting tumors. While some peptides encourage the growth and spread of tumor cells and angiogenic mechanisms, others display antitumor properties. As such, peptide ligands and receptor antagonists coul...

  • Review
  • Open Access
27 Citations
6,462 Views
17 Pages

Neurokinin-1 Receptor (NK-1R) Antagonists as a New Strategy to Overcome Cancer Resistance

  • Marilina García-Aranda,
  • Teresa Téllez,
  • Lauraine McKenna and
  • Maximino Redondo

30 April 2022

Nowadays, the identification of new therapeutic targets that allow for the development of treatments, which as monotherapy, or in combination with other existing treatments can contribute to improve response rates, prognosis and survival of oncologic...

  • Article
  • Open Access
8 Citations
3,705 Views
16 Pages

Harnessing the Anti-Nociceptive Potential of NK2 and NK3 Ligands in the Design of New Multifunctional μ/δ-Opioid Agonist–Neurokinin Antagonist Peptidomimetics

  • Charlène Gadais,
  • Justyna Piekielna-Ciesielska,
  • Jolien De Neve,
  • Charlotte Martin,
  • Anna Janecka and
  • Steven Ballet

6 September 2021

Opioid agonists are well-established analgesics, widely prescribed for acute but also chronic pain. However, their efficiency comes with the price of drastically impacting side effects that are inherently linked to their prolonged use. To answer thes...

  • Review
  • Open Access
15 Citations
6,228 Views
18 Pages

6 July 2015

Pancreatic cancer (PC) is the fourth leading cause of cancer related-deaths in both men and women, and the 1- and 5-year relative survival rates are 25% and 6%, respectively. It is known that smoking, alcoholism and psychological stress are risk fact...

  • Article
  • Open Access
3 Citations
2,754 Views
16 Pages

27 May 2022

Deoxynivalenol (DON), the most naturally-occurring trichothecenes, may affect animal and human health by causing vomiting as a hallmark of food poisoning. Deoxynivalenol-3-glucoside (D3G) usually co-occurs with DON as its glucosylated form and is ano...

  • Review
  • Open Access
30 Citations
4,933 Views
17 Pages

Acute myeloid leukemia (AML) is a heterogeneous hematological malignancy. To treat the disease successfully, new therapeutic strategies are urgently needed. One of these strategies can be the use of neurokinin-1 receptor (NK-1R) antagonists (e.g., ap...

  • Review
  • Open Access
3 Citations
2,979 Views
25 Pages

4 February 2025

Background: Diffuse intrinsic pontine glioma (DIPG) is a devastating childhood brainstem tumor. The median survival of DIPG is 16–24 months independent of the treatment received. Therefore, new therapeutic strategies against DIPG are urgently n...

  • Article
  • Open Access
5 Citations
2,566 Views
14 Pages

Substance P and Glucagon-like Peptide-17-36 Amide Mediate Anorexic Responses to Trichothecene Deoxynivalenol and Its Congeners

  • Hui Jia,
  • Zihui Qin,
  • Ben Wei,
  • Xinyi Guo,
  • Huiping Xiao,
  • Huayue Zhang,
  • Zelin Li,
  • Qinghua Wu,
  • Ruibo Zheng and
  • Wenda Wu

18 December 2022

Type B trichothecenes commonly contaminate cereal grains and include five structurally related congeners: deoxynivalenol (DON), 3-acetyldeoxynivalenol (3-ADON), 15-acetyldeoxynivalenol (15-ADON), fusarenon X (FX), and nivalenol (NIV). These toxins ar...

  • Article
  • Open Access
17 Citations
3,713 Views
15 Pages

31 July 2021

Although cisplatin is very effective as a treatment strategy in triple-negative breast cancer (TNBC), it has unwarranted outcomes owing to recurrence, chemoresistance and neurotoxicity. There is critically important to find new, effective and safe th...

  • Review
  • Open Access
1,073 Views
49 Pages

The Involvement of the Peptidergic Systems in Breast Cancer Development

  • Manuel L. Sánchez,
  • Prema Robinson,
  • Zal Italia,
  • Tan Hoang,
  • Miguel Muñoz and
  • Rafael Coveñas

14 November 2025

The current known data on the involvement of the peptidergic systems in breast cancer progression is overwhelmingly vast. Peptidergic systems are useful tools for imaging, diagnosis, prognosis and treatment of breast cancer. These systems play a cruc...

  • Article
  • Open Access
5 Citations
3,035 Views
15 Pages

Effects of Selective and Mixed-Action Kappa and Delta Opioid Receptor Agonists on Pain-Related Behavioral Depression in Mice

  • S. Stevens Negus,
  • Celsey M. St. Onge,
  • Young K. Lee,
  • Mengchu Li,
  • Kenner C. Rice and
  • Yan Zhang

16 July 2024

We recently developed a series of nalfurafine analogs (TK10, TK33, and TK35) that may serve as non-addictive candidate analgesics. These compounds are mixed-action agonists at the kappa and delta opioid receptors (KOR and DOR, respectively) and produ...

  • Article
  • Open Access
961 Views
14 Pages

Repeated Valproic Acid Administration Fundamentally Ameliorated Cisplatin-Induced Mechanical Allodynia in Rats

  • Yoshihiro Seto,
  • Yuki Ohara,
  • Manami Tachi,
  • Mari Tomonari,
  • Daisuke Inoue,
  • Fumiyasu Okazaki,
  • Yasuhiro Tsuji and
  • Hideto To

Cisplatin (cis-diamminedichloro-platinum; CDDP) is a chemotherapeutic agent that frequently induces peripheral neuropathy characterized by mechanical allodynia. Herein, we aimed to determine the effects of valproic acid (VPA) on cisplatin-induced mec...