Journal ArticleDOI
Some Aspects of the Pharmacology of Clemizole Hydrochloride
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TLDR
Clemizole was highly effective in antagonizing histamine aerosol bronchospasm and enhanced responses to epinephrine appear to be due to a sensitization to this amine by the antihistamine.Abstract:
Experiments have been described which demonstrate effective prolonged antihistaminic activity and other aspects of the pharmacology of clemizole HC1 (1- p -chloro-benzyl-2-pyrrolidyl-methyl-benzimidazole hydrochloride). A relatively high degree of antihistaminic specificity was observed in both in vitro and in vivo experiments. Clemizole was highly effective in antagonizing histamine aerosol bronchospasm. Spontaneous activity of isolated rabbit ileum and intestinal motility in anesthetized dogs were decreased. There was no significant effect on histamine-induced gastric secretion in chronic gastric fistula dogs. Enhanced responses to epinephrine appear to be due to a sensitization to this amine by the antihistamine. Acute and chronic studies showed a relatively low order of toxicity.read more
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Drug screening in Scn1a zebrafish mutant identifies clemizole as a potential Dravet syndrome treatment
TL;DR: Zebrafish Nav1.1 (scn1Lab) mutants originally identified in a chemical mutagenesis screen are characterised, representing a new direction in modeling pediatric epilepsy and could be used to identify novel therapeutics for any monogenic epilepsy disorder.
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Clemizole and modulators of serotonin signalling suppress seizures in Dravet syndrome
TL;DR: The findings demonstrate a rapid path from preclinical discovery in zebrafish, through target identification, to potential clinical treatments for Dravet syndrome, and it is demonstrated that clemizole binds to serotonin receptors and its antiepileptic activity can be mimicked by drugs acting on serotonin signalling pathways.
Journal ArticleDOI
Pharmaceutical policies: effects of cap and co-payment on rational use of medicines
Vera Lucia Luiza,Luisa Arueira Chaves,Rondineli Mendes da Silva,Isabel Cristina Martins Emmerick,Gabriela Costa Chaves,Silvia Cristina Fonseca de Araújo,Elaine L Moraes,Andrew D Oxman +7 more
TL;DR: Increasing the amount of money that people pay for medicines may reduce insurers' medicine expenditures and may reduce patients' medicine use, and the certainty of the evidence was found to be generally low to very low.
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The Hepatitis C Virus (HCV) NS4B RNA Binding Inhibitor Clemizole Is Highly Synergistic with HCV Protease Inhibitors
TL;DR: Clemizole can yield high-level synergy with the protease inhibitor class and inclusion in future anti-HCV cocktails can represent an attractive paradigm for increasing current virologic response rates.
Journal ArticleDOI
A Journey around the Medicinal Chemistry of Hepatitis C Virus Inhibitors Targeting NS4B: From Target to Preclinical Drug Candidates
TL;DR: The present review aims to discuss research published on NS4B functional inhibitors focusing the attention on hit identification, hit-to-lead optimization, ADME profile evaluation, and the structure-activity relationship data raised for each compound family taken into account.
References
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Journal Article
Comparative pharmacology of chlorpheniramine (chlor-trimeton) and its optical isomers
TL;DR: In vitro antihistamine studies on guinea pig gut have demonstrated that d -chlorpheniramine was approximately twice as potent as the racemic compound and the d -isomer in the anesthetized dog were similar to those of the dl -compound.
Journal Article
On the pharmacology of oxyphencyclimine hydrochloride.
TL;DR: Oxyphencyclimine was essentially the most potent in depressing gastric secretion and in preventing rumenal ulceration in rats and was the least potent in blocking other peripheral cholinergic activity as seen in both in vitro and in rico studies.