The amyloid Ab-42, a peptide involved, following a conformational change in b sheets in the pathology of the main neurodegenerative disorder of Alzheimer's disease, is targeted in our study, the latter of which reports the synthesis of two Inhibitors linked to a specific recognition sequence synthesized during this work (Tryp-Val-Val-COOH), one linked to an aziridine and the other to a methylated β-CD in order to be able to stop the aggregation of the peptide involved.
The surge in dopamine in ventral striatal regions in response to drugs of abuse and drug-associated stimuli is a final common pathway of addiction processes. GABA B agonists exert their effects indirectly, by quieting dopaminergic afferents. The ability of the GABA B agonist, baclofen ® to ameliorate nicotine and drug motivated behaviour, particularly with respect to its possible utility as a smoking cessation agent. This article provides a review of the use of baclofen ® in the treatment for different addiction. First, we present a brief overview of treatments of addictions for various substances of abuse, including alcohol, nicotine, and cocaine. Second part, summarizes the state of knowledge about the chemistry and toxicology of cigarette smoke. The section on "Chemistry" describes the chemical components of cigarette smoke and addresses aspects of product design. Finally, we come back to discuss some problems related to properties of baclofen ® that needs to be resolved, and our current investigation, to improve the therapeutic activity of baclofen ®. We conclude by an open question to doctors (addictologists and psychiatrists) hoping an answer as soon as possible.
Background: Baclofen® is an FDA-approved GABAB agonist, used for the treatment of spasticity since the early seventies. Objective: The aim of this study was to synthesize a new analog of BF. Methods: The main problem of baclofen® is that it is administered as a racemate. However, in our work we synthesize the R-(-) enantiomer. In our study, we used a stereoselective method for the synthesis of peptide analog and the study of their inclusion complex with CD, at the University of Tlemcen, Algeria in 2017. Results: For evaluation of anti-addiction activity, we have developed a new model in vivo, and the results are that our synthetized baclofen® analogues showed an anxiolytic effect. Regarding the toxicity, our results showed that our analogues have less toxic effect than baclofen; it reduces the activity of TGO enzymes, and TGP. From a histological point of view, it has no effect on the liver structure in addition to having a protective effect against lesions liverworts induced by alcohol. Conclusion: Our conclusion begs an open question: If baclofen® can cure any form of addiction such as smoking, alcoholism and other addictions to addictive substances, and if its beneficial effect is already proven, approved, and used as an anticraving agent in several countries in the world, why until now has the Algerian health community not used baclofen® in the treatment of numerous addictions?
Objective: The aim of this study was to synthesize new modified Cyclodextrins (CDs), for study of inclusion complex of drug with CD to improve water solubility. Methods: In this study, the formulation of bioactive molecules (Baclofen ® , aziridine synthesis and active propolis) with amphiphilic cyclodextrin (β-CD-amph) was prepared from native β-cyclodextrin (β-CD) via the simple co-precipitation method at the University of Tlemcen, Algeria (2016). Results: It was of interest to find a model of molecule derivatives that would be sufficiently water-stable and form a stable complex with (β-CD-amph) in aqueous medium, so that it could be used as a reference in future formulations or vectorization work. Among the nanoformulation, NMR studies of the inclusion complex of this derivative with b-cyclodextrin provided useful parameters related to the stoichiometry of the complex and the association with stant Ka. Conclusion: The geometry of the complex was assessed by 2D-ROESY experiments, suggesting a deep insertion of the guest into the cavity of (β-CD-amph).
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