Pharmacological and clinical overview of cloperastine in treatment of cough

Catania, Maria Antonietta; Cuzzocrea, Salvatore

doi:10.2147/tcrm.s16643

Cited by 16 publications

(6 citation statements)

References 17 publications

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“…Cloperastine ( Figure 5 , top left) is a cough-suppressant which acts to suppress the CNS cough center ( 56 ). Discovered in studies of derivatives of the first-generation antihistamine diphenhydramine ( Figure 5 , top right) ( 57 ), it also possesses antihistaminic activity. The SEA study suggested and experimentally confirmed binding of cloperastine to the sigma receptor, and noted that this could explain its antitussive activity, based on the known relationship of activity at the sigma receptor type 1 to cough ( 58 ).…”

Section: Resultsmentioning

confidence: 99%

Connecting proteins with drug-like compounds: Open source drug discovery workflows with BindingDB and KNIME

et al. 2015

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Today’s large, public databases of protein–small molecule interaction data are creating important new opportunities for data mining and integration. At the same time, new graphical user interface-based workflow tools offer facile alternatives to custom scripting for informatics and data analysis. Here, we illustrate how the large protein-ligand database BindingDB may be incorporated into KNIME workflows as a step toward the integration of pharmacological data with broader biomolecular analyses. Thus, we describe a collection of KNIME workflows that access BindingDB data via RESTful webservices and, for more intensive queries, via a local distillation of the full BindingDB dataset. We focus in particular on the KNIME implementation of knowledge-based tools to generate informed hypotheses regarding protein targets of bioactive compounds, based on notions of chemical similarity. A number of variants of this basic approach are tested for seven existing drugs with relatively ill-defined therapeutic targets, leading to replication of some previously confirmed results and discovery of new, high-quality hits. Implications for future development are discussed.Database URL: www.bindingdb.org

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Section: Resultsmentioning

confidence: 99%

Connecting proteins with drug-like compounds: Open source drug discovery workflows with BindingDB and KNIME

et al. 2015

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“…The regular clinical dose of cloperastine as a cough suppressant (10–20 mg three times daily for adults) is calculated to be approximately 3 µM. However, chronic toxicity tests performed in rats treated for 3 months with cloperastine hydrochloride at 15 mg/kg (45 µM) or 45 mg/kg (135 µM), and in dogs treated for 3 months with cloperastine hydrochloride at 20 mg/kg (60 µM) revealed no particular symptomatology or changes in hematochemical, hematological, or urinary parameters as compared to control animals and baseline values 10 . Thus, given the priority of cancer therapy, application of cloperastine to kill cisplatin-resistant cancer cells would be well within the scope of clinical testing.…”

Section: Discussionmentioning

confidence: 99%

Histamine H1 receptor antagonists selectively kill cisplatin-resistant human cancer cells

Matsumoto

Ebihara

Oishi

et al. 2021

Sci Rep

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Cancer therapy is often hampered by the disease’s development of resistance to anticancer drugs. We previously showed that the autonomously upregulated product of fibroblast growth factor 13 gene (FGF13; also known as FGF homologous factor 2 (FHF2)) is responsible for the cisplatin resistance of HeLa cisR cells and that it is likely responsible for the poor prognosis of cervical cancer patients treated with cisplatin. Here we show that cloperastine and two other histamine H1 receptor antagonists selectively kill HeLa cisR cells at concentrations that little affect parental HeLa S cells. The sensitivity of HeLa cisR cells to cloperastine was abolished by knocking down FGF13 expression. Cisplatin-resistant A549 cisR cells were similarly susceptible to cloperastine. H2, H3, and H4 receptor antagonists showed less or no cytotoxicity toward HeLa cisR or A549 cisR cells. These results indicate that histamine H1 receptor antagonists selectively kill cisplatin-resistant human cancer cells and suggest that this effect is exerted through a molecular mechanism involving autocrine histamine activity and high-level expression of FGF13. We think this represents a potential opportunity to utilize H1 receptor antagonists in combination with anticancer agents to treat cancers in which emergent drug-resistance is preventing effective treatment.

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“…4B, Translation), and sigma receptors such as Haloperidol 23 and Compound PB28 24 (Fig. 4A Nsp6 and Orf9c), Melperone, Cloperastine, 25 and Clemastine (Fig. 4B, Protein Processing), and the female hormone progesterone (Fig.…”

Section: Molecular Description Of Coronavirus Envelopementioning

confidence: 99%

Antiviral Drug-Membrane Permeability: the Viral Envelope and Cellular Organelles

Liu,

Elvati,

Violi

2020

Preprint

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To shorten the time required to find effective new drugs, like antivirals, a key parameter to consider is membrane permeability, as a compound intended for an intracellular target with poor permeability will have low efficacy. Here, we present a computational model that considers both drug characteristics and membrane properties for the rapid assessment of drugs permeability through the coronavirus envelope and various cellular membranes. We analyze 79 drugs that are considered as potential candidates for the treatment of SARS-CoV-2 and determine their time of permeation in different organelle membranes grouped by viral baits and mammalian processes. The computational results are correlated with experimental data, present in the literature, on bioavailability of the drugs, showing a negative correlation between fast permeation and most promising drugs. This model represents an important tool capable of evaluating how permeability affects the ability of compounds to reach both intended and unintended intracellular targets in an accurate and rapid way. The method is general and flexible and can be employed for a variety of molecules, from small drugs to nanoparticles, as well to a variety of biological membranes.

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Pharmacological and clinical overview of cloperastine in treatment of cough

Cited by 16 publications

References 17 publications

Connecting proteins with drug-like compounds: Open source drug discovery workflows with BindingDB and KNIME

Connecting proteins with drug-like compounds: Open source drug discovery workflows with BindingDB and KNIME

Histamine H1 receptor antagonists selectively kill cisplatin-resistant human cancer cells

Antiviral Drug-Membrane Permeability: the Viral Envelope and Cellular Organelles

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