Interesting Profile Research Articles

Sheep meat Beni-Guil breed: A local meat labeled PGI to promote quality and preserve biodiversity in Morocco

Currently, meat consumers are more conscious about the authentic meat products linked to their origin, which generates a growing demand for labeled sheep meat. In eastern Morocco, the Beni-Guil (BG) sheep meat is a Protected Geographical Indication (PGI) product. This study aimed to assess the variation of intramuscular fat quality of BG sheep in its cradles (Cr). The chemical composition of the longissimus lumborum muscle was evaluated from 20 female lambs obtained in the two main cradles of the BG breed (Ain Beni-Mathar (BG-Cr1) and Tendrara (BG-Cr2). The results show that the FA profile was affected by Cr (p<0.05). The oleic acid, palmitic acid, stearic acid, and linoleic acid are the dominants FA of analyzed meats. The polyunsaturated fatty acids (PUFA)/saturated fatty acids (SFA) and PUFA n-6/PUFAn-3 ratios respectively range from 1.15 and 5.02 for BG-sheep meats from Cr1 to 1.36 and 10.73 for those from Cr2. Overall, the results indicate that the analyzed meats have an interesting FAs profile with favorable ratios and indices. Thus, this study provides new information on the lipid quality of BG-IGP sheep meat produced extensively in two main cradles of this typical Moroccan sheep breed.

Prunella vulgaris L. seeds: a promising source of lipids, proteins, and original phenolic compounds presenting high antioxidant and anti-inflammatory activity

Description of the subject. Prunella vulgaris L. (Lamiaceae) is an edible herb used in Europe and Asia as herbal tea, food, dietary supplement or medicinal plant since several centuries. Although the composition and properties of the aerial parts are well documented in the literature, Prunella vulgaris seeds have never been investigated. Objectives. The aim of this work was to characterize the composition of these seeds to assess not only their nutritional potential (protein, lipid and minerals content), but also their antioxidant and anti-inflammatory potential as well as their specialized metabolites composition. Method. The protein, lipids and mineral content were determined. The phenolic compounds were isolated; elucidation of their structures was done by means of HR-MS and one- and two-dimensional NMR analysis. They were then evaluated for their biological activity, together with seed extracts. Results. Omega-3 rich oil and an interesting amino acids profile were detected in the seeds as well as the presence of a high content of polyphenolic compounds, including two structurally new compounds (phenylpropane derivatives) which were isolated and structurally characterized. The two compounds described here for the first time, were named amolsamic acids A&B. The seeds and amolsamic acids showed an interesting antioxidant potential, and a strong anti-inflammatory activity on neutrophils, MPO and HRP models. Conclusions. These findings highlight the real health promoting potential of P. vulgaris seeds and make them a good candidate as super-food or food supplement.

Total synthesis of bioactive tetracyclic norditerpene dilactones.

Tetracyclic norditerpene dilactones are an important class of terpenoids that have been isolated from both terrestrial and marine sources, typically from Podocarpus plants and from filamentous fungi. This class of molecules shares a common 6/6/6/5 tetracyclic ring skeleton, which possesses a densely oxygenated carbon framework and contiguous stereocenters. What's more challenging for synthetic chemists are the consecutive sp2-hybridized carbon centers, which exacerbates the strain/rigidity of the whole molecule. In addition, many of these molecules display promising biological activities, such as antitumor, insecticidal, anti-feedant, allelopathic, and antibiotic activities. The unique structures and interesting biological profiles of norditerpene dilactones have attracted considerable attention from synthetic chemists. Herein we summarize the synthetic efforts with respect to tetranorditerpene dilactones.

Pedagogy, Didactics, or Subject Matter? Exploring Pre-service Teachers’ Interest Profiles

Abstract Interest has been considered an important determinant of teacher quality. However, research into teacher interest, and more specifically, pre-service teachers’ interest is limited. Hence, the current study tackled the current gaps in pre-service teachers’ interest and aimed to explore pre-service teachers’ interest profiles based on the multidimensional framework of teacher interest. A total of 225 pre-service teachers, enrolled in various initial teacher education programs of two universities in Germany, participated voluntarily in the study. The results revealed two distinct pre-service teachers’ profiles based on the three teacher interest factors. Interestingly, the two profiles did not significantly differ in their subject interest levels, but did vary in their didactic and educational interest. In addition, the findings also revealed gender and school track differences in pre-service teachers’ interests and profiles. Consequences for future research and teacher education are discussed in detail.

Effects of dietary chromium-yeast level on growth performance, blood metabolites, meat traits and muscle fatty acids profile, and microminerals content in liver and bone of lambs

To assess the effect of dietary supplement levels of chromium-yeast (Cr-yeast) on growth performance, blood glucose and triglycerides, fatty acid (FA) profile in intramuscular fat, carcase and meat traits, iron, copper, chromium and zinc concentrations in liver and bone, 24 Rambouillet male lambs (29.2 ± 0.17 kg body weight) were randomly assigned to four diets with 0, 0.2, 0.4 and 0.6 mg Cr/kg DM. The growth performance trial lasted 49 d. Supplemental Cr-yeast did not affect growth performance and carcase characteristics (p > .05), but reduced (p < .05) perirenal and intramuscular fat, as well as 3 h post-feeding blood glucose and triglycerides concentration. In liver, Fe and Cu concentration decreased (p < .05), while Cr concentrations in liver increased with increasing Cr-yeast dietary levels. In bone, Fe decreased (p < .05) as Cr-yeast dietary levels increasing, and Cr-yeast supplementation increased Cr concentrations (p < .05). As Cr-yeast dietary level increased, palmitic (C16:0) and stearic (C18:0) SFA decreased linearly (p < .05), while palmitoleic (C16:1n-7), vaccenic (C18:1n-7), linoleic (C18:2n-6) and arachidic (C20:4) unsaturated fatty acids (UFA) increased linearly (p < .01). In conclusion, Cr-yeast did not affect growth performance and carcase quality, but decreased the perirenal and intramuscular fat, blood glucose and triglyceride content, and Fe and Cu concentrations in liver as increased Cr-yeast levels in the diet. Because supplemental Cr-yeast improved index of atherogenicity and unsaturated to saturated FA ratio in muscle of lambs, it could be of human nutritional interest. HIGHLIGHTS Cr-yeast supplementation reduced blood glucose and triglyceride concentration. In liver, Fe and Cu content decreased while Cr increased with increasing Cr-yeast dietary levels. Cr-yeast modified the FA profile of human nutritional interest and improved the unsaturated to saturated FA ratio in intramuscular fat.

Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer’s disease

In the present work, a novel series of pyridinethiazole bearing benzylpiperidine hybrids were designed and synthesized as dual-target inhibitors of GSK-3β/AChE. Among them, GD29 was the most promising candidate, with an IC50 value of 0.3 μM for hAChE and an IC50 value of 0.003 μM for hGSK-3β, respectively. The compounds exhibited good drug-like properties with optimal inhibitory enzyme activities. Moreover, GD29 showed anti-inflammatory properties at micromolar concentrations and displayed interesting neuroprotective profiles in an in vitro model of oxidative stress-induced neuronal death. Notably, the compounds also exhibited good permeability across the blood–brain-barrier (BBB) both in vitro. Central cholinomimetic activity was confirmed using a scopolamine-induced cognition impairment model in Institute of Cancer Research (ICR) mice upon oral administration. The current work identified optimized compounds and explored the therapeutic potential of glycogen synthase kinase 3/cholinesterase inhibition for the treatment of AD.

Multicriterial Evaluation of Renewable Energy Expansion Projects at Municipal Level for the Available Biomass Potential

To reduce emissions in the energy sector and reach worldwide climate goals, further expansion of renewable energy sources (RES) is inevitable. Local opposition has increased in recent years, resulting in the need for more consideration of acceptance issues in the planning process of RES projects. To fill this gap, a method is introduced to consider the dimension of social acceptance in a holistic approach and at an early project stage. In a two-step procedure, a municipal interest profile is created, followed by an examination of possible expansion projects based on the municipal profile. Both hard and soft characteristics of a given project are assessed in combination. Using the example of two potential scenarios for biomass expansion in a given municipality in Germany, the methodology is put to the test. The results show that with the new method House of municipal Energy (HomE), the interest profile of a municipality can be quantified in a comprehensible and transparent way. It is further shown that, depending on the initial objective function of the municipality, different expansion scenarios can be advantageous. In the examined case, the larger biogas plant achieves a higher utility value, since a clearly higher local added value can be generated. A smaller plant, which is only operated with waste materials, is preferable with regard to the required area and lower environmental impact. However, the advantages of the larger plant outweigh those of the smaller plant for the investigated example.

Chemical profile and biological properties of the endemic Turkish species Phyllocara aucheri

The aim of the present study is the phytochemical analysis of the aerial parts of Phyllocara aucheri (Boraginaceae), which is an endemic plant of Turkey. The phytochemical profile of the studied species was determined through LC-MS method. Sixteen secondary metabolites were identified, among which thirteen phenolic constituents, such as quercetin and kaempferol glycosides and caffeic acid derivatives, as well as three pyrrolizidine alkaloids (PAs) in the form of bases and N-oxides (PANOs) (europine, heliotrine and heliotrine N-oxide). The methanol extract of the aerial parts was assayed for its antioxidant properties, using free radical scavenging (DPPH•, ABTS•+), reducing power (FRAP, CUPRAC), phosphomolybdenum and metal chelating assays, while it has been also evaluated for in vitro enzyme inhibition against cholinesterases, α-amylase and α-glucosidase, exhibiting an interesting biological profile.

Novel quinazolin–sulfonamid derivatives: synthesis, characterization, biological evaluation, and molecular docking studies

In the design of novel drugs, the formation of hybrid molecules via the combination of several pharmacophores can give rise to compounds with interesting biochemical profiles. A series of novel quinazolin–sulfonamid derivatives (9a–m) were synthesized, characterized and evaluated for their in vitro antidiabetic, anticholinergics, and antiepileptic activity. These synthesized novel quinazolin–sulfonamid derivatives (9a–m) were found to be effective inhibitor molecules for the α-glycosidase, human carbonic anhydrase I and II (hCA I and hCA II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE) enzyme, with Ki values in the range of 100.62 ± 13.68–327.94 ± 58.21 nM for α-glycosidase, 1.03 ± 0.11–14.87 ± 2.63 nM for hCA I, 1.83 ± 0.24–15.86 ± 2.57 nM for hCA II, 30.12 ± 3.81–102.16 ± 13.87 nM for BChE, and 26.16 ± 3.63–88.52 ± 20.11 nM for AChE, respectively. In the last step, molecular docking calculations were made to compare biological activities of molecules against enzymes which are achethylcholinesterase, butyrylcholinesterase and α-glycosidase. Communicated by Ramaswamy H. Sarma

Cannabidiol: A Potential New Alternative for the Treatment of Anxiety, Depression, and Psychotic Disorders.

The potential therapeutic use of some Cannabis sativa plant compounds has been attracting great interest, especially for managing neuropsychiatric disorders due to the relative lack of efficacy of the current treatments. Numerous studies have been carried out using the main phytocannabinoids, tetrahydrocannabinol (THC) and cannabidiol (CBD). CBD displays an interesting pharmacological profile without the potential for becoming a drug of abuse, unlike THC. In this review, we focused on the anxiolytic, antidepressant, and antipsychotic effects of CBD found in animal and human studies. In rodents, results suggest that the effects of CBD depend on the dose, the strain, the administration time course (acute vs. chronic), and the route of administration. In addition, certain key targets have been related with these CBD pharmacological actions, including cannabinoid receptors (CB1r and CB2r), 5-HT1A receptor and neurogenesis factors. Preliminary clinical trials also support the efficacy of CBD as an anxiolytic, antipsychotic, and antidepressant, and more importantly, a positive risk-benefit profile. These promising results support the development of large-scale studies to further evaluate CBD as a potential new drug for the treatment of these psychiatric disorders.

Efficient chromatin accessibility mapping in situ by nucleosome-tethered tagmentation.

Chromatin accessibility mapping is a powerful approach to identify potential regulatory elements. A popular example is ATAC-seq, whereby Tn5 transposase inserts sequencing adapters into accessible DNA ('tagmentation'). CUT&Tag is a tagmentation-based epigenomic profiling method in which antibody tethering of Tn5 to a chromatin epitope of interest profiles specific chromatin features in small samples and single cells. Here, we show that by simply modifying the tagmentation conditions for histone H3K4me2 or H3K4me3 CUT&Tag, antibody-tethered tagmentation of accessible DNA sites is redirected to produce chromatin accessibility maps that are indistinguishable from the best ATAC-seq maps. Thus, chromatin accessibility maps can be produced in parallel with CUT&Tag maps of other epitopes with all steps from nuclei to amplified sequencing-ready libraries performed in single PCR tubes in the laboratory or on a home workbench. As H3K4 methylation is produced by transcription at promoters and enhancers, our method identifies transcription-coupled accessible regulatory sites.

In vitro protective effects of Paeonia officinalis var. mascula callus extract on human keratinocytes

Natural ingredients have been used to improve the state of health in humans. The genus Paeonia has been studied only limited yet it’s reported to have many activities such as antioxidant and anti-inflammatory. To this context, here we focused on an endemic Paeonia species in Attica. This study aims to present the development of the Paeonia officinalis var. mascula callus extract and its pleiotropic bioactivity on human primary keratinocytes exploring its potential application as an active agent in skin-related products. This extract showed a high scavenging activity with high phenolic content and an interesting metabolic profile. At a molecular level, the study on the transcript accumulation of genes revealed that this extract exhibits in vitro skin-related protection properties by mediating mitochondrial energy, cell proliferation, immune and inflammatory response and positively regulates genes involved in epidermal and in stratum corneum function. Besides, the extract is proven not skin irritant on reconstructed human skin model. These findings indicate that the specific P. officinalis var. mascula extract possesses significant in vitro protection activity on human epidermis and provides new insights into its beneficial role in skin confirming that the advent of biotechnology contribution the past few decades.

Calibration of Fiber Orientation Simulations for LFT—A New Approach

Short fiber reinforced thermoplastics (SFT) are extensively used due to their excellent mechanical properties and low processing costs. Long fiber reinforced thermoplastics (LFT) show an even more interesting property profile and are increasingly used for structural parts. However, their processing by injection molding is not as simple as for SFT, and their anisotropic properties resulting from the fiber microstructure (fiber orientation, length, and concentration) pose a challenge with regard to the engineering design process. To reliably predict the structural mechanical properties of fiber reinforced thermoplastics by means of micromechanical models, it is also necessary to reliable predict the fiber microstructure. Therefore, it is crucial to calibrate the underlying prediction models, such as the fiber orientation model, within the process simulation. In general, these models may be adjusted manually, but this is usually ineffective and time-consuming. To overcome this challenge, a new calibration method was developed to automatically calibrate the fiber orientation model parameters of the injection molding simulation by means of optimization methods. This optimization routine is based on experimentally determined fiber orientation distributions and leads to optimized parameters for the fiber orientation prediction model within a few minutes. To better understand the influence of the model parameters, different versions of the fiber orientation model, as well as process and material influences on the resulting fiber orientation distribution, were investigated. Finally, the developed approach to calibrate the fiber orientation model was compared with a classical approach, a direct optimization of the whole process simulation. Thereby, the new optimization approach shows a calculation time reduced by the factor 15 with comparable error variance.

Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3.

The members of the TRPML subfamily of non-selective cation channels (TRPML1-3) are involved in the regulation of important lysosomal and endosomal functions, and mutations in TRPML1 are associated with the neurodegenerative lysosomal storage disorder mucolipidosis type IV. For in-depth investigation of functions and (patho)physiological roles of TRPMLs, membrane-permeable chemical tools are urgently needed. But hitherto only two TRPML inhibitors, ML-SI1 and ML-SI3, have been published, albeit without clear information about stereochemical details. In this investigation we developed total syntheses of both inhibitors. ML-SI1 was only obtained as a racemic mixture of inseparable diastereomers and showed activator-dependent inhibitory activity. The more promising tool is ML-SI3, hence ML-SI1 was not further investigated. For ML-SI3 we confirmed by stereoselective synthesis that the trans-isomer is significantly more active than the cis-isomer. Separation of the enantiomers of trans-ML-SI3 further revealed that the (-)-isomer is a potent inhibitor of TRPML1 and TRPML2 (IC50 values 1.6 and 2.3μM) and a weak inhibitor (IC50 12.5μM) of TRPML3, whereas the (+)-enantiomer is an inhibitor on TRPML1 (IC50 5.9μM), but an activator on TRPML 2 and 3. This renders the pure (-)-trans-ML-SI3 more suitable as a chemical tool for the investigation of TRPML1 and 2 than the racemate. The analysis of 12 analogues of ML-SI3 gave first insights into structure-activity relationships in this chemotype, and showed that a broad variety of modifications in both the N-arylpiperazine and the sulfonamide moiety is tolerated. An aromatic analogue of ML-SI3 showed an interesting alternative selectivity profile (strong inhibitor of TRPML1 and strong activator of TRPML2).

Bioactive Ent-Kaurane Diterpenes Oridonin and Irudonin Prevent Cancer Cells Migration by Interacting with the Actin Cytoskeleton Controller Ezrin.

The ent-kaurane diterpene oridonin was reported to inhibit cell migration and invasion in several experimental models. However, the process by which this molecule exerts its anti-metastatic action has not been yet elucidated. In this article, we have investigated the anti-metastatic activity of Oridonin and of one homolog, Irudonin, with the aim to shed light on the molecular mechanisms underlying the biological activity of these ent-kaurane diterpenes. Cell-based experiments revealed that both compounds are able to affect differentiation and cytoskeleton organization in mouse differentiating myoblasts, but also to impair migration, invasion and colony formation ability of two different metastatic cell lines. Using a compound-centric proteomic approach, we identified some potential targets of the two bioactive compounds among cytoskeletal proteins. Among them, Ezrin, a protein involved in the actin cytoskeleton organization, was further investigated. Our results confirmed the pivotal role of Ezrin in regulating cell migration and invasion, and indicate this protein as a potential target for new anti-cancer therapeutic approaches. The interesting activity profile, the good selectivity towards cancer cells, and the lower toxicity with respect to Oridonin, all suggest that Irudonin is a very promising anti-metastatic agent.

Recovery of Bioactive Compounds from Hazelnuts and Walnuts Shells: Quantitative-Qualitative Analysis and Chromatographic Purification.

Hazelnut (HS) and walnut (WS) shells, an abundant by-product of the processing industries of these edible nuts, are traditionally considered as a low-value waste. However, they are a source of valuable compounds with an interesting chemical profile for the chemical and pharmaceutical sectors. In this study, the lipophilic and hydrophilic extracts present in HS and WS were quantified and identified, then the polar fractions were chromatographically separated, and their antioxidant capacity was studied. The experimental work includes the isolation of crude lipophilic and hydrophilic extracts by an accelerated extraction process, chromatographic analysis (gas chromatography-flame ionization (GC-FID), GC-mass spectroscopy (GC-MS), high-performance size-exclusion chromatography (HPSEC), thin-layer chromatography (TLC)), and quantification of the components. In addition, a thorough compositional characterization of the subgroups obtained by flash chromatography and their antioxidant capacity was carried out. The gravimetric concentrations showed different lipophilic/hydrophilic ratios (0.70 for HS and 0.23 for WS), indicating a higher proportion of polar compounds in WS than in HS. Moreover, the lipophilic extracts were principally composed of short-chain fatty acids (stearic, palmitic, and oleic acid), triglycerides, and sterols. The polar fractions were screened by thin-layer chromatography and then separated by flash chromatography, obtaining fractions free of fatty acids and sugar derivatives (97:3 in HS and 95:5 in WS), and mixtures richer in phenolic compounds and flavonoids such as guaiacyl derivatives, quercetin, pinobanksin, and catechin. The most polar fractions presented a higher antioxidant capacity than that of the crude extracts.

An Empirical Recommendation Framework to Support Location-Based Services

The rapid growth of Global Positioning System (GPS) and availability of real-time Geo-located data allow the mobile devices to provide information which leads towards the Location Based Services (LBS). The need for providing suggestions to personals about the activities of their interests, the LBS contributing more effectively to this purpose. Recommendation system (RS) is one of the most effective and efficient features that has been initiated by the LBS. Our proposed system is intended to design a recommendation system that will provide suggestions to the user and also find a suitable place for a group of users and it is according to their preferred type of places. In our work, we propose the Density-Based Spatial Clustering of Applications with Noise (DBSCAN) algorithm for clustering the check-in spots of the user’s and user-based Collaborative Filtering (CF) to find similar users as we are considering constructing an interest profile for each user. We also introduced a grid-based structure to present the Point of Interest (POI) into a map. Finally, similarity calculation is done to make the recommendations. We evaluated our system on real world users and acquired the F-measure score on average 0.962 and 0.964 for a single user and for a group of user respectively. We also observed that our system provides effective recommendations for a single user as well as for a group of users.

Consistency between personality career interest with sciences field among gifted and talented students

This research is conducted to identify the profiles of career personality and interest towards sciences field among the gifted and talented students (GTS) in Malaysia. The career interest tendency in science is based on the consistency according to Holland Three Letter Code (HTLC). A total of 213 GTS aged 15 to 17 years old were randomly selected to respond to Self-Directed Search–Form Easy (SDS) instrument. Data was collected through questionnaire distribution. Data were then analyzed using SPSS Window 23.0 and Excel 2010 software. The result from the study shows that out of six career interest personality, GTS demonstrate an inclination towards three personality characteristics which are Investigative ((𝑋̅=22.15), Social ((𝑋̅=19.88) and Artistic (𝑋̅=15.94). Based on the HTLC analysis, the study indicates a higher inclination towards sciences career interest (73.24%) as compared to non-sciences career interest (26.76%). “𝑋̅” for mean values and “%” for percentages. The findings also showed the existence of a mixed inclination on sciences and non-sciences or multi-potentiality among GTS. Its proven that GTS have a high sense of inquisitory which allows them to think scientifically and creative in finding solutions in their fields of interest.This study supports the past research findings that showed GTS have a high interest in sciences. The findings of this study have implications in the following areas; career counseling services, career guidance, and academic guidance to guide GTS on developing interest in science related fields of study.

Safety Profile and Adverse Events of Special Interest for Fruquintinib in Chinese Patients with Previously Treated Metastatic Colorectal Cancer: Analysis of the Phase3 FRESCO Trial.

In FRESCO (Fruquintinib Efficacy and Safety in 3+ Line Colorectal Cancer Patients) trial, fruquintinib demonstrated a statistically significant and clinically meaningful overall survival benefit in Chinese patients with metastatic colorectal cancer (mCRC). However, its safety profile, including adverse events of special interest (AESIs) and treatment-emergent adverse events (TEAEs) by age, sex, and body mass index (BMI), is not well known. The present analysis evaluated the safety profile and AESIs for fruquintinib in the FRESCO trial. In FRESCO, eligible Chinese patients were randomized (2:1) to receive fruquintinib (5mg once daily for 3weeks, followed by 1week off in 28-day cycles) or placebo plus best supportive care. Treatment-related AESIs and time to first occurrence of AESIs were summarized. Treatment-related TEAEs by age, sex, and BMI were also summarized. A total of 266 patients (95.7%) in the fruquintinib group and 97 (70.8%) in the placebo group had at least one treatment-related TEAE; the mean relative dose intensity was 92% and 98%, respectively. In the fruquintinib group, the most common (in > 40% of patients) treatment-related AESIs were hypertension (55.4%), palmar-plantar erythrodysesthesia syndrome [known as hand-foot skin reaction (HFSR)] (49.3%), and proteinuria (42.1%). The most common treatment-related grade ≥ 3 AESIs (≥ 3% of patients) were hypertension (21.2%), HFSR (10.8%), and proteinuria (3.2%); the median time to onset of these events was 10, 21, and 20days, respectively. Subgroup analysis by age, sex, and BMI revealed that the frequencies of treatment-related TEAEs were similar across all subgroups, and were consistent with the overall safety profile of fruquintinib. The most common treatment-related grade ≥ 3 AEs were hypertension, HFSR, and proteinuria. The treatment-related TEAE profile of fruquintinib in Chinese patents with mCRC was comparable among different subgroups and consistent with that reported in the overall population. Clinical Trials identifier NCT02314819.

Novel Highly Potent and Selective Sigma1 Receptor Antagonists Effectively Block the Binge Eating Episode in Female Rats.

In this paper, the benzo-cracking approach was applied to the potent sigma1 (σ1) receptor antagonist 1 to afford the less conformationally constrained 1,3-dioxane derivatives 2 and 3. To evaluate the effect of the increase in the distance between the two hydrophobic structural elements that flank the basic function, the cis and trans diastereomers of 4 and 5 were also prepared and studied. Compounds 2 and 3 showed affinity values at the σ1 receptor significantly higher than that of the lead compound 1. In particular, 3 displayed unprecedented selectivity over the σ2 receptor, the phencyclidine site of the NMDA receptor, and opioid receptor subtypes, as well as over the dopamine transporter. Docking results supported the structure–activity relationship studies. Due to its interesting biological profile, derivative 3, selected for an in vivo study in a validated preclinical model of binge eating, was able to counteract the overeating of palatable food only in binging rats, without affecting palatable food intake in the control group and anxiety-like and depression-related behaviors in female rats. This result strengthened the involvement of the σ1 receptor in the compulsive-like eating behavior and supported the σ1 receptor as a promising target for the management of eating disorders.