scholarly journals Possible Role of Exogenous Melatonin and Melatonin-Receptor-Agonists in the Treatment of Menopause―Associated Sleep Disturbances

2014 ◽  
Vol 04 (06) ◽  
pp. 309-320
Author(s):  
Amnon Brzezinski
Keyword(s):  
Sleep Disturbances ◽  
Melatonin Receptor ◽  
Exogenous Melatonin ◽  
Receptor Agonists ◽  
Melatonin Receptor Agonists

scholarly journals Insomnia in general practice: the role of doxylamine

2020 ◽  
pp. 45-53
Author(s):  
D. I. Burchakov ◽  
M. V. Tardov
Keyword(s):  
Clinical Case ◽  
Health Impact ◽  
Sleep Disruption ◽  
Melatonin Receptor ◽  
Chronic Patients ◽  
Receptor Agonists ◽  
Clinical Case Studies ◽  
Specialized Care ◽  
Melatonin Receptor Agonists

The general practitioner encounters all three forms of insomnia: idiopathic, chronic and acute. Idiopathic and chronic patients should receive specialized care by neurologist, psychiatrist or sleep disorders specialists because they require deep differential diagnosis and complex treatment. Acute insomnia patients need quick help to prevent the negative health impact and chronisation of sleep disruption. In theRussian Federation, the GP has access to three kinds of sleep drugs: benzodiazepines, melatonin receptor agonists, antihistamines. However, modern benzodiazepines are unavailable inRussiaand older benzodiazepines can lead to dependence. Melatonin receptor agonists are not effective enough for acute insomnia. Among available antihistamines, doxylamine is the most convenient option in clinical practice. Doxylamine has a good profile of safety and efficacy, it is included in the local clinical guidelines for insomnia. Also, doxylamine is the only sleep drug available for pregnant women. This paper presents a portrait of doxylamine and comments on its clinical niches and contraindications. We also discuss the pharmacology of doxylamine, drug interactions, and prescription modes. There are also three clinical case studies, presenting the typical acute insomnia patients and logic for their evaluation, underlining key clinical features of this disorder.

scholarly journals Cardioprotective Melatonin: Translating from Proof-of-Concept Studies to Therapeutic Use

2019 ◽  
Vol 20 (18) ◽  
pp. 4342 ◽  
Author(s):  
Ovidiu Constantin Baltatu ◽  
Sergio Senar ◽  
Luciana Aparecida Campos ◽  
José Cipolla-Neto
Keyword(s):  
Machine Learning ◽  
Heart Diseases ◽  
Safety Data ◽  
Proof Of Concept ◽  
Melatonin Receptor ◽  
Phase 3 ◽  
Therapeutic Role ◽  
Receptor Agonists ◽  
Melatonin Receptor Agonists

In this review we summarized the actual clinical data for a cardioprotective therapeutic role of melatonin, listed melatonin and its agonists in different stages of development, and evaluated the melatonin cardiovascular target tractability and prediction using machine learning on ChEMBL. To date, most clinical trials investigating a cardioprotective therapeutic role of melatonin are in phase 2a. Selective melatonin receptor agonists Tasimelteon, Ramelteon, and combined melatonergic-serotonin Agomelatine, and other agonists with registered structures in CHEMBL were not yet investigated as cardioprotective or cardiovascular drugs. As drug-able for these therapeutic targets, melatonin receptor agonists have the benefit over melatonin of well-characterized pharmacologic profiles and extensive safety data. Recent reports of the X-ray crystal structures of MT1 and MT2 receptors shall lead to the development of highly selective melatonin receptor agonists. Predictive models using machine learning could help to identify cardiovascular targets for melatonin. Selecting ChEMBL scores > 4.5 in cardiovascular assays, and melatonin scores > 4, we obtained 284 records from 162 cardiovascular assays carried out with 80 molecules with predicted or measured melatonin activity. Melatonin activities (agonistic or antagonistic) found in these experimental cardiovascular assays and models include arrhythmias, coronary and large vessel contractility, and hypertension. Preclinical proof-of-concept and early clinical studies (phase 2a) suggest a cardioprotective benefit from melatonin in various heart diseases. However, larger phase 3 randomized interventional studies are necessary to establish melatonin and its agonists’ actions as cardioprotective therapeutic agents.

scholarly journals Fluorine substituted methoxyphenylalkyl amides as potent melatonin receptor agonists

MedChemComm ◽  
2019 ◽  
Vol 10 (3) ◽  
pp. 460-464 ◽  
Author(s):  
Andrew Tsotinis ◽  
Rodanthi Kompogennitaki ◽  
Ioannis Papanastasiou ◽  
Peter J. Garratt ◽  
Alina Bocianowska ◽  
...  
Keyword(s):  
Side Chain ◽  
Melatonin Receptor ◽  
Receptor Agonists ◽  
Methoxy Groups ◽  
Melatonin Receptor Agonists

A series of fluorine substituted methoxyphenylalkyl amides were prepared with different orientations of the fluorine and methoxy groups with respect to the alkylamide side chain and with alkyl sides of differing lengths (n= 1–3).

The role of melatonin and melatonin receptor agonist in the prevention of sleep disturbances and delirium in intensive care unit – a clinical review

2020 ◽  
Vol 69 ◽  
pp. 127-134 ◽  
Author(s):  
Katarzyna Lewandowska ◽  
Marta A. Małkiewicz ◽  
Mariusz Siemiński ◽  
Wiesław J. Cubała ◽  
Paweł J. Winklewski ◽  
...  
Keyword(s):  
Intensive Care Unit ◽  
Intensive Care ◽  
Clinical Review ◽  
Receptor Agonist ◽  
Sleep Disturbances ◽  
Melatonin Receptor

Synthesis of a Novel Series of Benzocycloalkene Derivatives as Melatonin Receptor Agonists

2002 ◽  
Vol 45 (19) ◽  
pp. 4212-4221 ◽  
Author(s):  
Kohji Fukatsu ◽  
Osamu Uchikawa ◽  
Mitsuru Kawada ◽  
Toru Yamano ◽  
Masayuki Yamashita ◽  
...  
Keyword(s):  
Melatonin Receptor ◽  
Receptor Agonists ◽  
Melatonin Receptor Agonists
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