China
Africa
Explore chapters and articles related to this topic
Recent Cannabinoid Delivery Systems
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
Natascia Bruni, Carlo Della Pepa, Simonetta Oliaro-Bosso, Daniela Gastaldi, Franco Dosio, Enrica Pessione
Esposito et al. have described the development of a method to encapsulate cannabinoid drugs (precisely the inverse agonist of the CB1 receptor (AM251 and Rimonabant) and the URB597 fatty acid amide hydrolase inhibitor) in NLC [122]. In this circumstance, the lipid phase was composed of tristearin/tricaprylin 2:1 while Poloxamer 188 was added to the water phase. Nanoparticles of around 100 nm with high encapsulation efficiency were obtained.
Novel therapeutic and drug development strategies for tobacco use disorder: endocannabinoid modulation
Published in Expert Opinion on Drug Discovery, 2020
Increasing our understanding of the impact of anandamide reuptake inhibitors should also be a research focus given that they attenuate reinstatement of nicotine seeking and may also reduce nicotine self-administration, and some withdrawal signs. To date, the majority of research examining the effects of anandamide modulation has come from studies using FAAH inhibitors. Given the scarcity of studies with the reuptake inhibitors, it has been difficult to draw firm conclusions regarding their impact. An important consideration regarding anandamide reuptake inhibition relates to the potential for abuse. Squirrel monkeys self-administer the anandamide reuptake inhibitor AM404 [173] suggesting reuptake inhibitors may have some risk for abuse. In contrast, the FAAH inhibitor URB597 was not self-administered in squirrel monkeys [174] while the newer FAAH inhibitor URB694 was self-administered at a moderate rate [78]. Whether self-administration of AM404 represents a specific property of this compound or a more general drug class effect requires further research. Careful assessment of abuse risk will be required for both FAAH inhibitors and anandamide reuptake inhibitors going forward.
Effects of hypertension and FAAH inhibitor treatment of rats with primary and secondary hypertension considering the physicochemical properties of erythrocytes
Published in Toxicology Mechanisms and Methods, 2020
Izabela Dobrzyńska, Barbara Szachowicz-Petelska, Anna Pędzińska-Betiuk, Zbigniew A. Figaszewski, Elżbieta Skrzydlewska
Despite various literature data (positive/negative/no effect) on the effect of FAAH inhibitor (URB597) on the physiology and pathophysiology of living organisms, including hypertensive animals (Toczek et al. 2016; Biernacki, Ambrożewicz, et al. 2018; Martín Giménez et al. 2018), the effect of this compound on erythrocytes in both primary and secondary hypertension has not yet been analyzed. The results of this study indicate the positive effects of URB597 administration on both groups of rats with primary and secondary hypertension. URB597 normalizes the composition of the erythrocyte membrane and its physicochemical properties compared to the changes observed in hypertensive rats. Therefore, it can be suggested that URB597 has a beneficial effect on the structure of the membrane and thus on the functioning of erythrocytes. Therefore, despite the statement that URB597 does not normalize blood pressure during long-term administration, the compound may be a candidate for the active ingredient in potential preparations supporting the biological activity of erythrocytes, especially in diseases interfering with the functioning of these cells. In addition, it can be suggested that the assessment of the physicochemical properties of erythrocyte membranes can provide reliable and quick results useful for the effective assessment of erythrocyte status, which may consequently be a simple diagnostic tool.
Exploring the fatty acid amide hydrolase and cyclooxygenase inhibitory properties of novel amide derivatives of ibuprofen
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Alessandro Deplano, Jessica Karlsson, Mona Svensson, Federica Moraca, Bruno Catalanotti, Christopher J. Fowler, Valentina Onnis
In a key study from 2009, Naidu, Lichtman and colleagues2 reported that the ulcerogenic potency of the NSAID diclofenac was lower in mice lacking the enzyme fatty acid amide hydrolase (FAAH) than in the corresponding wild-type mice. A similar result was found in wild-type mice pre-treated with the irreversible FAAH inhibitor URB597 ((3′-(aminocarbonyl)[1,1′-biphenyl] − 3-yl)-cyclohexylcarbamate). Further, URB597 and diclofenac acted synergistically in reducing acetic acid-induced visceral nociception2. FAAH catalyses the hydrolysis of the endogenous cannabinoid (endocannabinoid) ligand anandamide (AEA, arachidonoylethanolamide)3 and the effects of FAAH inhibition upon diclofenac-induced ulceration were not seen in mice lacking cannabinoid-1 receptors2. The ability of FAAH inhibition to reduce the ulcerogenic potency of NSAIDs has also been seen with a peripherally-restricted FAAH inhibitor, URB937 (N-cyclohexyl-carbamic acid, 3′-(aminocarbonyl)−6-hydroxy[1,1′-biphenyl] − 3-yl ester) and with indomethacin as NSAID4. A second endocannabinoid, 2-arachidonoylglycerol (2-AG) is primarily hydrolysed by monoacylglycerol lipase, and inhibition of that enzyme also reduces the ulcerogenic potency of diclofenac5,6.