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Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

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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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An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
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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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Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

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Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
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Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

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Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
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Adrenergic Agonists: Indirect-Acting Agents01:25

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Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral...
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Small Molecule CXCR3 Antagonists.

Stephen P Andrews1, Rhona J Cox2

  • 1Heptares Therapeutics , BioPark, Broadwater Road, Welwyn Garden City, AL7 3AX, United Kingdom.

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|November 5, 2015
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Summary
This summary is machine-generated.

Small molecule chemokine receptor antagonists, particularly for CXCR3, show promise in treating inflammatory diseases. Further research into CXCR3 antagonists is needed for clinical development.

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Area of Science:

  • Immunology and Pharmacology
  • Drug Discovery and Development

Background:

  • Chemokines and their receptors are crucial in disease pathogenesis.
  • Despite numerous identified chemokine receptors, few antagonists are FDA-approved.
  • The chemokine receptor CXCR3 has emerged as a significant target in various diseases.

Purpose of the Study:

  • To review existing small molecule CXCR3 antagonists.
  • To explore the therapeutic potential of CXCR3 antagonists in inflammatory diseases.
  • To identify future opportunities for developing CXCR3 antagonists for clinical use.

Main Methods:

  • Literature review of published studies on CXCR3 antagonists.
  • Analysis of preclinical efficacy data for CXCR3 antagonists.
  • Assessment of the clinical trial landscape for CXCR3 antagonists.

Main Results:

  • Several classes of small molecule CXCR3 antagonists have been developed.
  • Two CXCR3 antagonists demonstrated efficacy in preclinical models of inflammation.
  • Only one CXCR3 antagonist has advanced to clinical trials.

Conclusions:

  • Significant opportunities exist for developing novel CXCR3 antagonists.
  • Further investigation of known CXCR3 antagonist classes is warranted.
  • Targeting CXCR3 offers a promising avenue for treating inflammatory conditions.