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CNS Receptors for Opioids
Published in Edythe D. London, Imaging Drug Action in the Brain, 2017
Richard J. Knopp, Mary Hunt, James K. Wamsley, Henry I. Yamamura
The human experience of pain consists of both cognitive (subjective) and sensory components which together influence the effectiveness of analgesic treatment (Cervero, 1985). Animal investigations of analgesia focus on antinociception or the behavioral response to aversive environmental stimuli that, depending on the subject used, may depend less on cognitive neural systems (Kavaliers, 1988). This distinction leaves open the possibility that higher level supraspinal systems may play an important role in human analgesia without having a corresponding role in different experimental animals. Thus, opioid receptive neurons in cortical and limbic brain areas may influence human analgesia to a greater extent than is suggested by animal experiments. However, it is also important to note the strong correlation between opioid analgesic activity observed in human clinical studies with antinociceptive activity measured using animal models (Taber, 1974).
Ameliorative potential of flavonoids of Aegle marmelos in vincristine-induced neuropathic pain and associated excitotoxicity
Published in Nutritional Neuroscience, 2021
Mrinmoy Gautam, Muthiah Ramanathan
Different parts of A. marmelos are used for various conditions like anaemia, asthma, high blood pressure, swollen joints, diabetes, hyperlipidemia etc. [3]. Its antinociception activity mediates through opioid and monoaminergic pain pathways, suggesting its effect on chronic neuropathic pain. The umbelliferone (β-D-galactopyranoside) possesses anti-diabetic effect in streptozotocin-induced diabetic rats through increase in pancreatic insulin secretion and antioxidant regulation [4]. Aegle marmelos extracts also shown enhanced glycemic control and regeneration of the β-cells of the pancreas [5]. The literature indicates the medicinal value of various parts of A. marmelos and р-coumaric acid in suppressing monosodium urate-crystal induced inflammation in rats [6]. Marmelosin is one of the active principles of A. marmelos and has shown antioxidant, anti-inflammatory, and anticancer properties via TNF-α mediated Akt signalling pathway [7].
Chronic High-Dose Buprenorphine Does Not Block Subjective High from Diacetylmorphine in a Patient in Heroin-Assisted Treatment
Published in Journal of Psychoactive Drugs, 2019
Marc Vogel, Patrick Köck, Johannes Strasser, Gerhard Wiesbeck, Marc Walter, Kenneth M. Dürsteler
Theoretically, an even higher dose of BUP might be necessary to completely block full agonist effects as suggested by Greenwald, Comer, and Fiellin (2014). However, we refrained from raising the dose above 48 mg per day because increasing sedation (which has been reported to be a κ-agonist effect (Brust et al. 2016; Zhang et al. 2015)) under the combination of high-dose BUP with IV DAM was observed clinically and self-reported by the patient. Increased agonist effects may seem counterintuitive but have been reported for the combination of BUP and morphine for antinociception in pain treatment (Beltrutti and Niv 2000; Beltrutti et al. 2002), albeit in much lower doses (van Niel, Schneider, and Tzschentke 2016). Clearly, the high DAM dose must have contributed strongly to the sedation observed.
HYPNOTIZABILITY-RELATED FAAH C385A POLYMORPHISM: POSSIBLE ENDOCANNABINOID CONTRIBUTION TO SUGGESTION-INDUCED ANALGESIA
Published in International Journal of Clinical and Experimental Hypnosis, 2020
Silvano Presciuttini, Giancarlo Carli, Enrica L. Santarcangelo
Scarce information is available regarding the contribution of various neurotransmitters to the cognitive control of pain in highly hypnotizabile subjects (highs). The inefficacy of naloxone administration in the suppression of their suggestion-induced analgesia indicates that the release of endogenous opioids cannot be responsible for it (Moret et al., 1991). In addition, the opioid receptor μ1 polymorphism, which is more frequently observed in highs, is the one associated with low responsiveness to opiates (Presciuttini et al., 2018). This makes the opioid contribution to both cognitively and physically induced antinociception quite unlikely in highs (Fidanza et al., 2017).