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R Ceserani

Publications and source records attributed to R Ceserani.

58 records · Page 4Linked to original sources
PubMedDate not supplied

Effects of naftopidil on some urodynamic parameters and arterial blood pressure in comparison with prazosin in conscious rats.

Naftopidil, an alpha 1-adrenergic antagonist, was orally tested in comparison with prazosin, in a rat cystomanometric model to evaluate the effect on the bladder volume capacity (BVC), the micturition pressure (MP) and the mean arterial blood pressure (MAP), contemporaneously recorded to evaluate the selectivity of action. Naftopidil induced a clearcut increase of BVC and a decrease of MP without lowering MAP at 6.25 mg kg-1 p.o.. Prazosin was inactive on BVC, decreased MP and induced a significant decrease of MAP at 1.56 mg kg-1 p.o. Naftopidil could offer an advantage when compared with prazosin.

Adrenergic alpha-Antagonists↗
PubMedDate not supplied

Stereoselective pharmacokinetics of moguisteine metabolites in healthy subjects.

We studied the pharmacokinetics of moguisteine, a racemic non-narcotic peripheral antitussive drug, in 12 healthy male subjects after a single oral administration of 200 mg. The unchanged drug was absent in plasma and urine of all subjects. Moguisteine was immediately and completely hydrolyzed to its main active metabolite, the free carboxylic acid M1. Therefore, we evaluated the kinetic profiles of M1, of its enantiomers R(+)-M1 and S(-)-M1, and of M1 sulfoxide optical isomers M2/I and M2/II by conventional and stereospecific HPLC. Maximum plasma concentrations for M1 (2.83 mg/l), M2/I (0.26 mg/l) and M2/II (0.40 mg/l), were respectively reached at 1.3, 1.6 and 1.5 h after moguisteine administration. Plasma concentrations declined after the peak with mean apparent terminal half-lives of 0.65 h (M1), 0.88 h (M2/I) and 0.84 h (M2/II). Most of the administered dose was recovered in urine within 6 h from moguisteine treatment. The systemic and renal clearance values indicated high renal extraction ratio for all moguisteine metabolites, and particularly for M1 sulfoxide optical isomers. Plasma concentration-time profiles and urinary excretion patterns for M1 enantiomers R(+)-M1 and S(-)-M1 were quite similar. Thus, for later moguisteine pharmacokinetic evaluations the investigation of the plasma concentration-time curve and the urinary excretion of the sole racemic M1 through non-stereospecific analytical methods may suffice in most cases.

Administration, Oral↗
PubMedDate not supplied

Byciclic compounds with potential antiulcer and/or antisecretory activity. III--2-substituted tetrahydrothiazolo-[5,4-c]pyridines.

As the ultimate result of a long-term search for new bicyclic molecules potentially endowed with antiulcer and/or antisecretory activity, simple urea derivatives of 2-guanidino-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine [(VIII), Fig. 1; X = 0, R = alkyl], displaying a strong inhibition of stress- and ASA-induced gastric ulcers and of basal gastric secretion, were found. Their potency does compare very favourably with that of cimetidine and ranitidine and approaches that of famotidine. On spontaneously beating guinea pig atria they behaved as inhibitors of the histamine H2-receptor. In contrast with cimetidine and ranitidine but like other recently described inhibitors (famotidine included), the most active compounds (VIII) caused a surmountable antagonism only at low concentrations and an unsurmountable antagonism at higher concentrations. The onset of action was slow, while the inhibitory effect was hardly reversed by washing. The rational development of the research and the synthetic approach, as well as a quantitative assessment of both in vitro and in vivo potencies in comparison with the best known, clinically used drugs, are shown in detail.

Animals↗