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Peripheral Neuropathy
Published in Charles Theisler, Adjuvant Medical Care, 2023
Palmitoylethanolamide (PEA): Many patients suffering from neuropathic conditions have pain that is refractory to existing treatments. In this context, palmitoylethanolamide (PEA), an endogenous fatty acid amide, is emerging as a novel agent in the treatment of pain and inflammation.16 Palmitoylethanolamide is available as a supplement (PeaPure and PeaPlex) and as a cream (PEA cream).
Pharmacotherapy of Neurochemical Imbalances
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Rupali Patil, Aman Upaganlawar, Suvarna Ingale
The interesting fact observed was that though cannabinoids exist only naturally in plant with no biological connection in humans, many parts of brain, namely cerebral cortex, basal ganglia, cerebellum, and hippocampus express huge numbers of receptors for cannabinoids. This made scientific workers to think of endogenous substances which may be selectively interacting with CB and whose action is facilitated by Delta-9-tetrahydrocannabinol. Thus in 1992, the first endogenous ligand of CB1 receptors later labeled as Anandamide was discovered in porcine brain. The name, Anandamide was derived from the Sanskrit word ‘Ananda’ meaning ‘Bliss.’ With the discovery of anandamide, many other metabolites collectively termed as endocannabinoids, were characterized and discovered to act as useful agonists of CB in the brain, however they were not superior in efficacy than anandamide (Devane et al., 1992). The endocannabinoids are found in the brain or other tissues only in small amounts. Similar to other lipid mediators, they are formed and released locally on call. Anandamide and endocannabinoids are rapidly inactivated by reuptake through transporter and by metabolism through the enzyme fatty acid amide hydrolase. The anandamide is formed from the precursor N-arachidonic phosphatidyl ethanolamine by hydrolysis in presence of an enzyme phosphodiesterase enzyme phospholipase D (Iversen, 2003).
Endocannabinoid System & Cannabinoid Receptors
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
Fatty acid amide hydrolase (FAAH) is a main gatekeeper in cardiac functions, substance abuse disorders, and regulation of nociception [11–14]. Cell culture and animal studies have shown inhibiting FAAH may be a treatment option in anxiety disorders [15]. Certain flavonoids have been found to inhibit FAAH in its effort to break down the endocannabinoid anandamide [16]. Anandamide is responsible for maintaining basic endocannabinoid signaling. FAAH inhibition increases endocannabinoid concentrations and decreases pro-inflammatory cytokines while increasing the production of anti-inflammatory cytokines [10].
Metabolomics approach of Symphyotrichum squamatum ethanol extract and its nano-Ag formulation protective effect on gastric ulcer via bio-chemical and pathological analyses
Published in Biomarkers, 2023
Heba A. Hassan, Iriny M. Ayoub, Tamer I. M. Ragab, Sherif M. Afifi, Abd El-Nasser G. El-Gendy, Abdel Razik H. Farrag, Ahmed M. Abd-ELGawad, Mohamed Farag, Abdelsamed Elshamy, Naglaa M. Ammar
In this study, potential biomarkers associated with various metabolic pathways related to GU were identified using metabolomics in disease rat serum. According to multivariate data analysis, lipids, energy metabolism, pyrimidine and phosphatidylinositol signalling system pathway were the most influential. Interestingly, fatty acid amides (FAAs) form a group of endogenous lipid mediators of growing interest in their biological role. FAAs can be divided into two classes: fatty acid primary amides and N-acyl-ethanolamines (Hiley and Hoi 2007). An interesting result of the present study is that oleamide, which is a primary fatty acid amide was lowered in the serum of ulcer model group (Figure 4B). Oleamide is the prototype long-chain primary fatty acid amide lipid messenger (Mueller and Driscoll 2009) produced from oleoylglycine, or from the direct amidation of oleic acid via oleoyl coenzyme A by cytochrome c using ammonia as the nitrogen source. In a prior study, it was reported that ulcer model group showed reduced oleamide levels related to invasive inflammation (Ammar et al.2022).
Emerging drugs for the treatment of bladder storage dysfunction
Published in Expert Opinion on Emerging Drugs, 2022
The cannabinoid (CB) receptors, their endogenous ligands and related enzymes for biosynthesis and degradation constitutes the endocannabinoid system [22,83,84]. From the cannabis plant cannabinoids (phytocannabinoids) can be extracted. The main compounds in such extracts are THC, cannabidiol, and cannabinol. Two G-protein-coupled CB receptors have been defined: type 1 (CB1) and type 2 (CB2). The G-protein-coupled receptor 55 (GPR55), has been described as a third CB receptor, but its pharmacology is incompletely known. Endocannabinoids and ‘exocannabinoids,’ such as phyto-cannabinoids and synthetic cannabinoids, interact with these receptors and some associated endogenous fatty acid amides (FAA). Within the endocannabinoid system at least two major arachidonate-derived ligands, anandamide, and 2-arachidonoylglycerol (2-AG), mediate their effects by binding to CB1 and CB2 receptors. Both anandamide and 2-AG act extensively in the central and peripheral nervous system. They affect not only LUT function but may influence pain, mood, feeding behavior, motivation, and inflammation [85–87].
Non-clinical toxicology evaluation of BIA 10-2474
Published in Critical Reviews in Toxicology, 2021
A. Wallace Hayes, Klaus Weber, Paul Moser, Patrício Soares-da-Silva
The clinical trial with BIA 10-2474 was a first-in-man Phase I trial with single-ascending (SAD) and multiple-ascending dose (MAD) phases. During the SAD phase doses of 100 mg demonstrated no safety concerns and during the MAD phase, 10 days of 20 mg were similarly well tolerated (Rocha et al. 2016). Inhibition of FAAH increases the levels of several fatty acid amides including anandamide, the endogenous ligand of cannabinoid receptors. Although the primary therapeutic target was analgesia, FAAH inhibitors have been suggested for multiple therapeutic uses and several have been tested in the clinic, with no signs of adverse effects (Li et al. 2012; Pawsey et al. 2016; Postnov et al. 2018). Although directly acting cannabinoid agonists are associated with side effects such as hypothermia, sedation, and impaired memory and attention (De Vry et al. 2004; Toczek and Malinowska 2018) it is expected that indirectly increasing cannabinoid tone by inhibiting FAAH will be devoid of these side-effects.