New opioid receptor modulators and agonists

Kaye, Alan D.; Cornett, Elyse M.; Patil, Shilpa; Gennuso, Sonja A.; Colontonio, Matthew M.; Latimer, Dustin; Kaye, Aaron J.; Urman, Richard D.; Vadivelu, Nalini

doi:10.1016/j.bpa.2018.06.009

Cited by 9 publications

(3 citation statements)

References 52 publications

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“… 3 The µ-opioid receptor is in a family of G-protein–coupled receptors that, when activated, modulate presynaptic and postsynaptic calcium channels, attenuating the excitability of neurons. 4 …”

Section: Introductionmentioning

confidence: 99%

Low-dose naltrexone’s utility for non-cancer centralized pain conditions: a scoping review

2023

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Background At low doses, naltrexone (LDN) has been shown to modulate inflammation through the interruption of microglial cell activation within the central nervous system. One of the most likely contributors to centralized pain is changes in microglial cell processing, therefore, it has been postulated that LDN can be used to manage patients with pain resulting from central sensitization due to this relationship. This scoping review aims to synthesize the relevant study data for LDN as a novel treatment strategy for various centralized pain conditions. Methods A comprehensive literature search was conducted using PubMed, Embase, and Google Scholar guided by the Scale for Assessment of Narrative Review Articles (SANRA) criteria. Results 47 studies related to centralized pain conditions were identified. Many of the studies were case reports/series and narrative reviews, however a few RCTs have been conducted. Overall, the body of evidence revealed improvement in patient-reported pain severity as well outcomes related to hyperalgesia, physical function, quality of life, and sleep. Variability in dosing paradigms and the time to patient response was present in the reviewed studies. Conclusions Evidence synthesized for this scoping review supports the ongoing use of LDN for the treatment of refractory pain in various centralized chronic pain conditions. Upon review of the current available published studies, it is apparent that further high-quality, well-powered RCTs need to be conducted in order to establish efficacy, standardization for dosing, and determine response times. In summary, LDN continues to offer promising results in the management of pain and other distressing symptoms in patients with chronic centralized pain conditions.

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Section: Introductionmentioning

confidence: 99%

Low-dose naltrexone’s utility for non-cancer centralized pain conditions: a scoping review

2023

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“…A local community traditionally uses the leaves of this plant to treat different diseases like fever, muscle pain, diarrhea, toughs, malarial, high blood pressure, diabetes mellitus, and worm diseases. 2 Some studies have reported a pharmacological activity of M. speciosa leaves such as antinociceptive, 3,4 antiinflammation, 5 analgesic, 6,7 opioid-like effects, 8,9 and morphine withdrawal effect. 10,11 However, legality is still constrained in its utilization related to the sedative effect caused by the high content of indole alkaloids.…”

Section: Introductionmentioning

confidence: 99%

Green and Optimum Extraction of Total Polyphenols Content from Mitragyna speciosa Korth. Havil Leaves using Microwave- Assisted Natural Deep Eutectic Solvent Extraction

Prabowo¹,

Agustina²,

Nur³

et al. 2022

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The current study mainly aims to apply and optimize the microwave-assisted natural deep eutectic solvent extraction (MANDESE) method of total polyphenol content from Mitragyna speciosa (Korth.) Havil leaves using response surface methodology (RSM) and its extraction mechanism using scanning electron microscopy (SEM) imaging. The extraction process was performed using the maceration and MANDESE method. Total polyphenols content was examined using Folin-Ciocalteu reagent and spectrophotometer UV-Vis. The extraction mechanism was performed using SEM imaging. The extraction condition as experimental design variable factors for optimization using RSM included NADES composition ratio, the liquid-solid ratio, extraction time, and microwave power. The results show that the MANDESE with some different combinations of NADES composition is more effective than a maceration. SEM imaging result shows that the levels of damage of cells and cell walls were more severe after extraction. The optimum extraction condition has obtained the NADES composition ratio of 3 g/g (choline chloride/sorbitol) and the liquid-solid ratio of 20 mL/g for 20 min extraction time with 60% Watts microwave power. The scale-up confirmation test was obtained the total polyphenols content of 526.12 µg GAE/g sample. This finding demonstrated the optimum condition of the MANDESE method and performed efficiently, rapidly, safely, and environmentally friendly.

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“…However, the experience to modulate the opioid system in the ocular surface is more limited. The use of known exogenous opioids [ 20 ] and the pharmacology synthesis of new agonists, antagonists, or modulators of opioid receptors [ 21 ] holds the possibility for manipulation of these pathways and the finding of new targeted therapies for common ocular surface problems like delayed corneal wounds, dry eye disease, and neuropathic and chronic ocular pain.…”

Section: Introductionmentioning

confidence: 99%

Opioids and Ocular Surface Pathology: A Literature Review of New Treatments Horizons

García-López

Gómez-Huertas

Sánchez‐González

et al. 2022

JCM

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This review discusses the role of opioids in the corneal surface and the different pathways and therapeutic methods of management. A literature review was performed using PubMed database. For the database search, the main searching words “opioid” and “topical opioid treatment” were used with the descriptors “cornea”, “ocular surface”, “neuropathic corneal pain”, “corneal sensitivity” and “naltrexone”; original scientific articles and reviews were included to achieve the purpose of the review. The endogenous opioid system has relevant functions in the organism, and in daily use, opioids are used as painkillers. However, these drugs may be employed for other indications as opioid pathways have a wide spectrum. The corneal surface for topical treatment is easily accessible, hence sparing the side effects of systemic opioids. Instillation of opioid antagonist substances, such as naltrexone, increases corneal healing rates and stimulates the division of corneal epithelium cells without deleterious effects. The natural modulation of endogenous opioids controls different forms of pain, including inflammatory and neuropathic pain, both in the ocular surface and in the central nervous system. There are diverse methods in controlling pain using opioids, especially in refractory forms. This review attempts to collect the literature about corneal surface and opioid pathways to provide an overview image and a possible direction of the news treatments.

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New opioid receptor modulators and agonists

Cited by 9 publications

References 52 publications

Low-dose naltrexone’s utility for non-cancer centralized pain conditions: a scoping review

Low-dose naltrexone’s utility for non-cancer centralized pain conditions: a scoping review

Green and Optimum Extraction of Total Polyphenols Content from Mitragyna speciosa Korth. Havil Leaves using Microwave- Assisted Natural Deep Eutectic Solvent Extraction

Opioids and Ocular Surface Pathology: A Literature Review of New Treatments Horizons

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