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Clinical, Retrospective data, Journal: Not first-line antihypertensive agents, but still effective-The efficacy and safety of imidazoline receptor agonists: A network meta-analysis. (Pubmed Central) - May 29, 2024
Moreover, moxonidine reduced blood pressure more effectively than enalapril; however, this difference was not significant (SBP MD: 3.10; 95% CI: -2.60-8.80; DBP MD: 1.30; 95% CI: -1.25-3.85)...After 8?weeks of treatment, the appearance of dry mouth was highest with clonidine (OR: 9.27 95% CI: 4.70-18.29) and lowest with rilmenidine (OR: 6.46 95% CI: 0.85-49.13) compared to placebo...However, in the case of resistant hypertension, they are a viable option. According to our findings, from the point of view of safety and efficacy, moxonidine appears to be the best choice among imidazoline receptor agonists.
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Synthesis of rilmenidine analogues as potential therapeutic agents for the treatment of breast cancer | Poster Board #1612 (In-person; Poster Board #1612; Hall C (Ernest N. Morial Convention Center)) - Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_2959;
To this end the synthesis of a broad series of rilmenidine analogues has been initiated to establish the structure activity relationships of this molecule relative to Nischarin activation. To achieve the preparation of the initial target compounds, new chemistry has been explored for the efficient synthesis of the N-(2- chloroethyl)urea precursors to the target amino-oxazoline analogues.
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Review, Journal: New anti-aging strategies: a narrative review. (Pubmed Central) - Dec 25, 2023
Age-related protein crosslinks are acknowledged as a causative factor in age-related diseases. Anti-aging medicine is an evolving field with a multitude of drugs and strategies, necessitating further clinical studies and long-term follow-up based on clinical experience and insights gained from delayed adverse events.
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Journal: Autophagy and anti-inflammation ameliorate diabetic neuropathy with Rilmenidine. (Pubmed Central) - Dec 11, 2023
Anti-aging medicine is an evolving field with a multitude of drugs and strategies, necessitating further clinical studies and long-term follow-up based on clinical experience and insights gained from delayed adverse events. The findings of this study suggest that Rilmenidine may have therapeutic effects on DNP by modulating antioxidant and autophagic pathways.
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Journal: The Role of Autophagy in Chemical Proteasome Inhibition Model of Retinal Degeneration. (Pubmed Central) - Aug 7, 2021
These results suggest that Becn1-mediated autophagy is not an effective intrinsic protective mechanism for retinal damage induced by insults, including impaired proteasomal activity; furthermore, autophagic activation beyond normal levels is required to alleviate the cytotoxic effect of proteasomal inhibition. Further studies are underway to delineate the precise roles of different forms of autophagy, and investigate the effects of their activation in rescuing retinal neurons under various pathological conditions.
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Journal: Deciphering Imidazoline Off-Targets by Fishing in the Class A of GPCR field. (Pubmed Central) - Jul 11, 2021
Therefore, to investigate possible off-target effects of imidazoline ligands we have prepared a reverse docking protocol on class A GPCRs, using imidazoline ligands and their decoys. To verify our in silico results, three ligands with high scores and three ligands with low scores were tested for antagonistic activity on α2- adrenoceptors.
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[VIRTUAL] Nischarin as a target for drug repurposing in solid tumors () - May 30, 2021 - Abstract #EACR2021EACR_999;
Conclusion NISCH is potentially a good candidate as a target for drug repurposing in solid tumors. Our future efforts will include validation of NISCH prognostic role in solid tumors and extensive preclinical examination of the mechanisms by which NISCH agonists exert their anticancer properties.
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[VIRTUAL] Nischarin as a target for drug repurposing in solid tumors () - May 30, 2021 - Abstract #EACR2021EACR_998;
Conclusion NISCH is potentially a good candidate as a target for drug repurposing in solid tumors. Our future efforts will include validation of NISCH prognostic role in solid tumors and extensive preclinical examination of the mechanisms by which NISCH agonists exert their anticancer properties.
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[VIRTUAL] Nischarin as a target for drug repurposing in solid tumors () - May 30, 2021 - Abstract #EACR2021EACR_997;
Conclusion NISCH is potentially a good candidate as a target for drug repurposing in solid tumors. Our future efforts will include validation of NISCH prognostic role in solid tumors and extensive preclinical examination of the mechanisms by which NISCH agonists exert their anticancer properties.
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[VIRTUAL] Nischarin as a target for drug repurposing in solid tumors () - May 30, 2021 - Abstract #EACR2021EACR_996;
Conclusion NISCH is potentially a good candidate as a target for drug repurposing in solid tumors. Our future efforts will include validation of NISCH prognostic role in solid tumors and extensive preclinical examination of the mechanisms by which NISCH agonists exert their anticancer properties.
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Review, Journal: Autophagy in neurodegeneration: New insights underpinning therapy for neurological diseases. (Pubmed Central) - Dec 17, 2020
We summarize studies pinpointing mitophagy mediated by the serine/threonine kinase PINK1 and the ubiquitin-protein ligase Parkin as a mechanism potentially relevant to Parkinson's disease, despite debate over the physiological conditions in which it is activated in organisms. Finally, with the example of the autophagy-inducing agent rilmenidine and its discrepant effects in cell culture and mouse models of motor neuron disorders, we illustrate the importance of considering aspects such a disease stage and aggressiveness, type of insult and load of damaged or toxic cellular components, when choosing the appropriate drug, timepoint and duration of treatment.
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Review, Journal: Imidazoline Receptor System: The Past, the Present, and the Future. (Pubmed Central) - Sep 22, 2020
Existing data suggest that I receptors may represent a binding site at the Kir6.2-subtype ATP-sensitive potassium channels in pancreatic β-cells and may be involved in insulin secretion. Despite the elusive nature of their molecular identities, recent progress on drug discovery targeting imidazoline receptors (I and I) demonstrates the exciting potential of these compounds to elicit neuroprotection and to treat various disorders such as hypertension, metabolic syndrome, and chronic pain.
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Journal: Cardiovascular Effects Mediated by Imidazoline Drugs: an Update. (Pubmed Central) - Jul 4, 2020
Currently, new imidazoline receptors ligands are in development. In the present review, we provide a brief update on the cardiovascular effects of clonidine, moxonidine, rilmenidine, and the novel imidazoline agents since representing an important therapeutic target for some cardiovascular diseases.
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Journal: Potential Therapeutic Use of Neurosteroids for Hypertension. (Pubmed Central) - Jan 12, 2020
This focused review examines the possibility that neurosteroids may be a novel therapeutic approach to address the neurogenic contribution to hypertension. We discuss the causes and prevalence of neurogenic hypertension, current therapeutic approaches, and the applicability of using neurosteroids as antihypertensive therapy.
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Journal: Synergism of myocardial β-adrenoceptor blockade and I-imidazoline receptor-driven signaling: Kinase-phosphatase switching. (Pubmed Central) - Dec 20, 2019
Direct measurements of phosphatase activity in the myocardial tissues showed that activation of the IRs leads to stimulation of STPP, which could be responsible for the I-agonist influences. Obtained data clarify peripheral effects that occur during activation of the IRs under endogenous catecholaminergic stress, and can be used in clinical practice for more precise control of heart contractility in some cardiovascular pathologies.
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Journal: Sympathetic neurotransmission in spleens from aging Brown-Norway rats subjected to reduced sympathetic tone. (Pubmed Central) - Oct 8, 2019
Despite the rilmenidine-induced increase in β-AR expression, splenocyte c-AMP production was comparable with age-matched controls, thus dampening nerve activity had no effect on receptor coupling to adenylate cyclase. Understanding how aging affects neuroimmune regulation in healthy aging rodent models may eventually lead to strategies that improve health in aging populations vulnerable to immunosenescence and low-grade systemic inflammation.
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Journal: Non-Central Influences of α2-Adrenergic and Imidazoline Agonist Interactions in Isolated ardiomyocytes Cardiac Cells (Pubmed Central) - May 25, 2019
We propose that the coordinated activation of autophagic flux and lysosomal biogenesis contribute to the effective clearance of dysfunctional mitochondria by rapamycin. obtained data make it possible to formulate a number of useful recommendations for clinical practice, and also to clarify the non-central peripheral effects arising from the activation of α2‑adrenergic or imidazoline systems under conditions of endogenous hyperactivation on of the two systems.
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Enrollment change: Sympathetic Nerve Activity in Renal Failure (clinicaltrials.gov) - Mar 17, 2015
P4, N=0, Withdrawn,
These findings suggest that rilmenidine treatment may drive disease progression and neurodegeneration in this mouse model due to excessive mitophagy, implying that alternative strategies to beneficially stimulate autophagy are warranted in ALS. N=80 --> 0
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