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New glutaramic acid derivatives with potent competitive and specific cholecystokinin-antagonistic activity.
TLDR
New glutaramic acid derivatives were evaluated for anti-cholecystokinin activity in vitro on guinea pig gallbladder, causing a parallel right shift of the cumulative dose-response curve of the agonist. Expand
Pharmacokinetics of dexloxiglumide after administration of single and repeat oral escalating doses in healthy young males.
TLDR
The pharmacokinetics, safety and tolerability of dexloxiglumide, a new CCK1 receptor antagonist currently under development for the treatment of the constipation-predominant irritable bowel syndrome, were evaluated by standard noncompartmental methods. Expand
Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists.
TLDR
In vivo lorglumide antagonizes the contraction of the gall bladder of the guinea pig and of the dog provoked by i.v. CCK-8, and is protective against ceruletide-, taurocholate- and diet-induced pancreatitis and is a candidate for diagnostic or therapeutic use in man when an involvement of CCK is suspected. Expand
Characterization of antisecretory and antiulcer activity of CR 2945, a new potent and selective gastrin/CCK(B) receptor antagonist.
TLDR
The results suggest that CR 2945 might be a promising compound for the therapy of acid-related disorders, and that its clinical use could help clarify the therapeutic potential of gastrin/CCK(B) receptor antagonists in the gut. Expand
CR 2945: a novel CCKB receptor antagonist with anxiolytic-like activity.
TLDR
The results suggest that CR 2945 might be a promising alternative to the existing therapy of anxiety-related disorders. Expand
Effect of Three Nonpeptide Cholecystokinin Antagonists on Human Isolated Gallbladder
TLDR
Examining the effect of dexloxiglumide on isolated human gallbladder contraction induced by cholecystokinin–octapeptide and comparing this effect to that of lorglumide and amiglumides shows that the three molecules have a potent antagonistic effect, of a competitive nature, on gallbladders choleCystokin in type 1 receptors. Expand
Pharmacological profile of CR3465, a new leukotriene CysLT1 receptor antagonist with broad anti-inflammatory activity.
TLDR
It is concluded that CR3465 represents a potent leukotriene CysLT1 receptor antagonist with enhanced effects, being also useful for counteracting spasmogenic and inflammatory stimuli other than those elicited by cysteinyl-leukotrienes (Cys-LTs). Expand
Characterization of antigastrin activity in vivo of CR 2194, a new R-4-benzamido-5-oxo-pentanoic acid derivative.
TLDR
The interaction of CR 2194 with the gastrin receptors appeared reversible, as demonstrated by the return to normal values of the acid output after the conclusion of the i.v. infusion, during pentagastrin continuous stimulation in the dog. Expand
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory
TLDR
The tacrine-related heterobivalent ligand 6o was designed in an attempt to capitalize on the evidence of a certain degree of conformational freedom of the amino acid residues interacting with the substituents in positions 3 and 4 of the quipazine quinoline nucleus, and represents the first example of a rationally designed high-affinity 5-HT(3) receptor ligand showing nanomolar AChE inhibitory activity. Expand
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
TLDR
Qualitative and quantitative structure-affinity relationship studies carried out by making use of theoretical molecular descriptors allowed to elucidate the role of the main pharmacophoric components and to develop a model for the interaction of the 5-HT3 ligands related to quipazine with their receptor. Expand
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