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Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates...
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5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
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Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
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Neurokinin 3 receptor antagonism - the magic bullet for hot flushes?

Climacteric : the journal of the International Menopause Society·2017
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Neurokinin 3 receptor antagonists - prime time?

J K Prague1,2

  • 1Macleod Diabetes and Endocrine Centre, Royal Devon and Exeter Hospital, Exeter, UK.

Climacteric : the Journal of the International Menopause Society
|November 2, 2020
PubMed
Summary

New treatments targeting the neurokinin B/NK3 receptor pathway offer effective relief for menopausal hot flashes. These NK3 receptor antagonists provide a promising alternative to hormone therapy for women experiencing vasomotor symptoms.

Keywords:
Neurokinin 3 receptor antagonistshot flushesmenopausenovel therapeuticsvasomotor symptoms

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Area of Science:

  • Reproductive endocrinology and neurobiology
  • Pharmacology of novel therapeutics

Background:

  • Vasomotor symptoms, including hot flashes and night sweats, significantly impact menopausal women's quality of life.
  • Current treatments like hormone therapy have risks and contraindications, necessitating alternative solutions.
  • The neurokinin B (NKB)/neurokinin 3 receptor (NK3R) pathway is implicated in the development of these symptoms.

Purpose of the Study:

  • To evaluate the efficacy and tolerability of NK3 receptor antagonists for treating menopausal vasomotor symptoms.
  • To explore a non-hormonal therapeutic option for managing hot flashes.

Main Methods:

  • Clinical trials involving chemically distinct oral NK3R antagonists.
  • Assessment of symptom reduction and side effect profiles.

Main Results:

  • Consistent demonstration of efficacy across multiple clinical trials.
  • Favorable tolerability profiles reported for NK3R antagonists.
  • Significant reduction in the frequency and severity of hot flashes.

Conclusions:

  • NK3 receptor antagonists are a promising, effective, and well-tolerated non-hormonal treatment for menopausal vasomotor symptoms.
  • These agents may offer a safe alternative for women unable to use or seeking alternatives to hormone therapy.
  • Further large-scale studies are warranted to confirm long-term efficacy and safety for widespread clinical adoption.