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Pharmaceuticals
Special Issues
Discovery and Development of Novel Analgesics
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Discovery and Development of Novel Analgesics

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 25 May 2025 | Viewed by 3866

Special Issue Editors

Dr. Ethel Antunes Wilhelm

E-Mail Website
Guest Editor
Graduate Program in Biochemistry and Bioprospecting, Biochemical Pharmacology Research Laboratory, Federal University of Pelotas, Pelotas 96010-900, RS, Brazil
Interests: pain; neuropathy; oxidative stress; selenium; inflammation
Dr. Angélica Schiavom dos Reis

E-Mail Website
Guest Editor
Graduate Program in Biochemistry and Bioprospecting, Biochemical Pharmacology Research Laboratory, Federal University of Pelotas, Pelotas 96010-900, RS, Brazil
Interests: pre-clinical models; aging; pain; oxaliplatin-induced neuropathy; pathophysiological mechanisms

Special Issue Information

Dear Colleagues,

The International Association for the Study of Pain (IASP) revised the definition of pain in 2020 to "an unpleasant sensory and emotional experience associated with, or resembling that associated with, actual or potential tissue damage". Pain affects billions of people globally and is a significant challenge to global health due to its associated disability and mortality. Chronic pain impacts autonomy, sleep, social activities, and employment, making effective pain management a major challenge in modern medicine.

The quest for novel analgesics remains a key focus in biomedical research, driven by the need to alleviate pain. Current analgesics, including non-steroidal anti-inflammatory drugs (NSAIDs), opioids, and adjuvant therapies, have limitations, such as gastrointestinal toxicity, addiction potential, and inadequate efficacy in chronic pain conditions. Therefore, there is an urgent need for novel analgesics that provide effective pain relief with fewer side effects. Technological advancements and a deeper understanding of pain biology drive the discovery and development of new analgesics, including the identification of novel molecular targets, the synthesization and screening of potential compounds, and the translation of preclinical findings into clinical practice. Innovative methodologies enhance the efficiency and precision of analgesic development. Continued collaboration and innovation are essential to meeting the clinical need for safer and more effective pain management options, ultimately improving patient outcomes and quality of life.

For this Special Issue, we invite authors to submit original and review articles on preclinical and clinical findings that enhance our understanding of novel analgesics, with the aim of compiling research from leading experts, emphasizing therapeutic agents and strategies, and identifying future directions for effective pain management innovation and therapies.

Dr. Ethel Antunes Wilhelm
Dr. Angélica Schiavom dos Reis
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • analgesics
  • pain management
  • pain biology
  • pharmacological potential
  • preclinical models
  • therapeutic development
  • synthetic compounds
  • natural compounds
  • neuropathic pain
  • chemotherapy-induced neuropathy

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (2 papers)

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Research

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27 pages, 4842 KiB  
Article
Discovery of a Novel Multitarget Analgesic Through an In Vivo-Guided Approach
by Guo Zhen, Nayeon Do, Nguyen Van Manh, Hee-Jin Ha, Hee Kim, Hyunsoo Kim, Kwanghyun Choi, Jihyae Ann and Jeewoo Lee
Pharmaceuticals 2025, 18(2), 205; https://doi.org/10.3390/ph18020205 - 3 Feb 2025
Viewed by 1058
Abstract
Background: Pain is a complex condition influenced by peripheral, central, immune, and psychological factors. Multitarget approaches offer a more effective and safer alternative to single-target analgesics by enhancing efficacy, reducing side effects, and minimizing tolerance. This study aimed to identify a novel multitarget [...] Read more.
Background: Pain is a complex condition influenced by peripheral, central, immune, and psychological factors. Multitarget approaches offer a more effective and safer alternative to single-target analgesics by enhancing efficacy, reducing side effects, and minimizing tolerance. This study aimed to identify a novel multitarget analgesic with improved pharmacological properties. Methods: An in vivo-guided screening approach was used to discover a new analgesic compound. Compound 29, derived from a novel scaffold inspired by opiranserin and vilazodone pharmacophores, was identified through analog screening in the formalin test. Its efficacy was further evaluated in the spinal nerve ligation (SNL) model of neuropathic pain. Mechanistic studies explored its interaction with neurotransmitter transporters and receptors, while pharmacokinetic and safety assessments were conducted to determine its stability, brain penetration, and potential toxicity. Results: Compound 29 demonstrated high potency in the formalin test, with an ED50 of 0.78 mg/kg in the second phase and a concentration-dependent effect in the first phase. In the SNL model, it produced dose-dependent analgesic effects, increasing withdrawal thresholds by 24% and 45% maximum possible effect (MPE) at 50 and 100 mg/kg, respectively. Mechanistic studies revealed strong triple uptake inhibition, particularly at dopamine (DAT) and serotonin (SERT) transporters, alongside high-affinity 5-HT2A receptor antagonism. Pharmacokinetic analysis indicated enhanced stability and blood–brain barrier permeability. In vitro studies confirmed its nontoxicity to HT-22 cells but revealed potential hERG inhibition and strong CYP3A4 inhibition. Conclusions: Compound 29 is a promising multitarget analgesic with potent efficacy and favorable pharmacokinetics. Ongoing optimization efforts aim to mitigate side effects and enhance its therapeutic profile for clinical application. Full article
(This article belongs to the Special Issue Discovery and Development of Novel Analgesics)
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Review

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23 pages, 2708 KiB  
Review
Emerging Psychotropic Drug for the Treatment of Trigeminal Pain: Salvinorin A
by Geovanna Nallely Quiñonez-Bastidas, Lucia Elhy Grijalva-Contreras, Selene Isabel Patiño-Camacho and Andrés Navarrete
Pharmaceuticals 2024, 17(12), 1619; https://doi.org/10.3390/ph17121619 - 30 Nov 2024
Cited by 1 | Viewed by 2235
Abstract
Trigeminal neuralgia (TN) is chronic pain caused by damage to the somatosensorial system on the trigeminal nerve or its branches, which involves peripheral and central dysfunction pain pathways. Trigeminal pain triggers disruptive pain in regions of the face, including within and around the [...] Read more.
Trigeminal neuralgia (TN) is chronic pain caused by damage to the somatosensorial system on the trigeminal nerve or its branches, which involves peripheral and central dysfunction pain pathways. Trigeminal pain triggers disruptive pain in regions of the face, including within and around the mouth. Besides clinical experiences, translating the language of suffering into scientific terminology presents substantial challenges. Due to the complex and multifactorial pathophysiology underlying trigeminal pain, elucidating its social impact presents significant difficulties. Carbamazepine and oxcarbazepine are first-line treatments for TN, achieving approximately 50% pain reduction in 60–70% of treated patients. However, their efficacy is often limited by common side effects, such as dizziness, vertigo, nausea, seizures, and cognitive symptoms. In some cases, patients experience severe side effects, including myelosuppression, hyponatremia, hormonal imbalances, liver toxicity, suicidal ideation, teratogenicity, and other adverse reactions. Given these clinical limitations, the search for new painkiller candidates continues. Hence, we focused this review on salvinorin A (SalA), a natural agonist of κ-opioid receptors (KORs), which demonstrated anti-nociceptive, anti-inflammatory, and anti-neuropathic properties in various experimental models of the spinal sensory system. Furthermore, preclinical evidence indicates that SalA does not induce dependence and demonstrates a favorable toxicological and safety profile in comparison with currently marketed opioid drugs. We propose Salvinorin A as a promising candidate for treating trigeminal neuralgia, offering the potential for reduced adverse effects. Full article
(This article belongs to the Special Issue Discovery and Development of Novel Analgesics)
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