Results 171 to 180 of about 4,187 (189)

MAGL inhibitor NanoMicellar formulation (MAGL-NanoMicellar) for the development of an antiglaucoma eye drop

International Journal of Pharmaceutics, 2022
The ocular endocannabinoid system (ECS) including enzymes and CB1/CB2 receptors determines various substantial effects, such as anti-inflammatory activity and reduction of the intraocular pressure (IOP). The modulation of 2-arachidonoylglycerol (2-AG) levels obtained via MAGL inhibition is considered as a promising pharmacological strategy to activate ...
Patrizia Chetoni, Susi Burgalassi, Erica Zucchetti, Carlotta Granchi, Filippo Minutolo, Silvia Tampucci, Daniela Monti   +6 more
openaire   +3 more sources

Identification and characterization of a new reversible MAGL inhibitor

Bioorganic & Medicinal Chemistry, 2014
Monoacylglycerol lipase is a serine hydrolase that play a major role in the degradation of 2-arachidonoylglycerol, an endocannabinoid neurotransmitter implicated in several physiological processes. Recent studies have shown the possible role of MAGL inhibitors as anti-inflammatory, anti-nociceptive and anti-cancer agents.
TUCCINARDI, TIZIANO, GRANCHI, CARLOTTA, Rizzolio F, Caligiuri I, Battistello V, Toffoli G, MINUTOLO, FILIPPO, MACCHIA, MARCO, MARTINELLI, ADRIANO   +8 more
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A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013-2017)

Expert Opinion on Therapeutic Patents, 2017
Monoacylglycerol lipase is a serine hydrolase that plays a major role in the degradation of the endocannabinoid 2-arachidonoylglycerol. Because of this key role, selective inactivation of MAGL represents an interesting approach to obtain desirable effects in several diseases.
Carlotta Granchi, Isabella Caligiuri, Filippo Minutolo, Flavio Rizzolio, Tiziano Tuccinardi   +4 more
openaire   +4 more sources

Monoacylglycerol lipase (MAGL) as a promising therapeutic target

Biochemical Pharmacology, 2018
Monoacylglycerol lipase (MAGL) has been characterized as the main enzyme responsible for the inactivation of the most abundant brain endocannabinoid, 2-arachidonoylglycerol (2-AG). Besides this role, MAGL has progressively acquired a growing importance as an integrative metabolic hub that controls not only the in vivo levels of 2-AG but also of other ...
Ana, Gil-Ordóñez, Mar, Martín-Fontecha, Silvia, Ortega-Gutiérrez, María L, López-Rodríguez   +3 more
openaire   +3 more sources

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Loratadine analogues as MAGL inhibitors

Bioorganic & Medicinal Chemistry Letters, 2015
Compound 12a (JZP-361) acted as a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46 nM), and was found to have almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50=7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50=1.79 μM).
Jayendra Z, Patel, Stephen, Ahenkorah, Miia, Vaara, Marek, Staszewski, Yahaya, Adams, Tuomo, Laitinen, Dina, Navia-Paldanius, Teija, Parkkari, Juha R, Savinainen, Krzysztof, Walczyński, Jarmo T, Laitinen, Tapio J, Nevalainen   +11 more
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The Role of Monoacylglycerol Lipase (MAGL) in the Cancer Progress

Cell Biochemistry and Biophysics, 2014
In recent years, metabolism is talked highly important in cancer research, especially the lipid metabolism. Researchers believe that the de novo fatty acid synthesis plays an important role in tumor development, while many studies illustrated that Endocannabinoids have anti-tumorigenic actions, including anti-proliferation, apoptosis induction, and ...
Hong, Qin, Zhi-hua, Ruan
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Systemic and spinal administration of FAAH, MAGL inhibitors and dual FAAH/MAGL inhibitors produce antipruritic effect in mice

Archives of Dermatological Research, 2016
The increase of endocannabinoid tonus by inhibiting fatty acid amide hydrolase (FAAH) or monoacylglycerol lipase (MAGL) represents a promising therapeutic approach in a variety of disease to overcome serious central side effects of exocannabinoids. Recent studies reported that systemic administration of FAAH and MAGL inhibitors produce antipruritic ...
Ozgur, Yesilyurt, Mutlu, Cayirli, Yusuf Serdar, Sakin, Melik, Seyrek, Ahmet, Akar, Ahmet, Dogrul   +5 more
openaire   +2 more sources

Model predictive control of magle system

2017 International Conference on Innovations in Green Energy and Healthcare Technologies (IGEHT), 2017
Model predictive control (MPC), which works on the basis of receding horizon control has attracted the process control community due to its capability to grasp constraints on process variables, nonlinearities plus interactions among process variables, disturbances etc.
D. Periyasamy, M. Germin Nisha
openaire   +1 more source