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Highly potent and selective ligands for histamine H3-receptors
New drugs selective for histamine H3-receptors can be used to establish that these receptors are involved in the feedback control ofhistamine synthesis and release, and to demonstrate theirExpand
BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, Hydrochloride], a Nonimidazole Inverse Agonist/Antagonist at the Human Histamine H3 Receptor: Preclinical Pharmacology
TLDR
Preclinical data suggest that BF2.649 is a valuable drug candidate to be developed in wakefulness or memory deficits and other cognitive disorders. Expand
The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice
TLDR
Thiorphan is reported here that this compound, thiorphan [(DL-3-mercapto-2-benzylpropanoyl)-glycine; patent no. 8008601] protects the enkephalins from the action of enkephalinase in vitro in nanomolar concentration and in vivo after either intracerebroventricular or systemic administration. Expand
Efficacy and tolerability of racecadotril in acute diarrhea in children.
TLDR
This study demonstrates the efficacy (up to 50% reduction in stool output) and tolerability of racecadotril as adjuvant therapy to oral rehydration solution in the treatment of severe diarrhea in infants and children. Expand
Effects of acetorphan, an enkephalinase inhibitor, on experimental and acute diarrhoea.
TLDR
The efficacy and tolerance of acetorphan suggest that enkephalinase inhibition may represent a novel therapeutic approach for the symptomatic management of acute secretory diarrhoea without impairing intestinal transit. Expand
An inverse agonist of the histamine H3 receptor improves wakefulness in narcolepsy: Studies in orexin−/− mice and patients
TLDR
H(3)-receptor inverse agonists could constitute a novel effective treatment of EDS, particularly when associated with modafinil, a currently-prescribed wake-promoting drug. Expand
Pitolisant versus placebo or modafinil in patients with narcolepsy: a double-blind, randomised trial
TLDR
Pitolisant at doses up to 40 mg was efficacious on EDS compared with placebo and well tolerated compared with modafinil, and could offer a new treatment option for patients with narcolepsy. Expand
Safety and efficacy of pitolisant on cataplexy in patients with narcolepsy: a randomised, double-blind, placebo-controlled trial
TLDR
Pitolisant was well tolerated and efficacious in reducing cataplexy and might constitute a useful first-line therapy for catapLexy in patients with narcolepsy, for whom there are currently few therapeutic options. Expand
Effect of sinorphan, an enkephalinase inhibitor, on plasma atrial natriuretic factor and sodium urinary excretion in cirrhotic patients with ascites.
TLDR
Enkephalinase inhibition transiently increases sodium urinary excretion in cirrhotic patients with ascites via a mechanism that is likely to imply reduction of ANF catabolism, suggesting that ANF could play a role in the control of sodium homeostasis in liver cirrhosis with ascite. Expand
Bioavailability, antinociceptive and antiinflammatory properties of BP 2-94, a histamine H3 receptor agonist prodrug.
TLDR
From its pharmacokinetics and pharmacological profile BP 2-94 appears to be a promising novel therapeutic agent in disorders such as asthma, migraine or a variety of inflammatory diseases and pain associated with these disorders. Expand
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