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Biomedical subjects

L Rossini

Publications and source records attributed to L Rossini.

At least 55 records · Page 3Linked to original sources

The usefulness, in pharmacological classification, of complementary pattern-recognition techniques and structure modelling as afforded by the iterative collation of multiple-trial data in data banks.

In this emerging information age no significant limits can be envisaged to the immense resources of knowledge that pharmacological sciences can draw upon by systematically applying multivariate pattern-recognition techniques to those data banks which can be organized internationally with better standardization of descriptors, i.e. by parametrizing observations and evaluating monitoring in experimental, biological assays, clinical trials and postmarketing surveillance. Even conventionally or habitually adopted references and communalities such as traditional drug profiles and receptor models may be iteratively re-checked and suitably adapted so as to take account of more adequate, up-to-date analytical techniques, fresh biological ideas and new advances in terms of physiological refinements. An attempt may also be made to modify the chemicophysical relationships and patterns currently traced on the basis of what are held to be quantitative structure-activity oversimplifications. The present paper focuses upon specifying a number of standardization criteria in conventional assays and upon submitting multiple biological features to monitoring; in addition, it gives some picture of the new trends the approach can offer and draws attention to the more relevant, innovative literature references.

Animals↗

Electrophysiological analysis of the cholinergic effects of cimetidine and ranitidine.

The study takes the form of an analysis of the effects of cimetidine and ranitidine (2 x 10(-4) M) on 9 electrophysiological parameters, using a single frog sciatic nerve-sartorius muscle preparation. The parameters evaluated were: (i) mean end-plate potential (e.p.p.) amplitude, and mean 50%-corrected e.p.p. amplitude, (ii) mean rise time (RT), (iii) mean half-decay (HD), (iv) mean miniature end-plate potential (m.e.p.p.) amplitude, (v) mean resting membrane potential (RMP), (vi) mean m.e.p.p. frequency (f), (vii) mean quantal content (m), (viii) quantum release probability (p), and (ix) number of active sites (n) in the nerve terminal. Marquardt analysiswas used in order to determine the effects of cimetidine and raniditine on end-plate potential kinetics. At the concentration assayed only ranitidine showed a marked blocking effect at postsynaptic level as well as a less pronounced presynaptic effect. The time course of the e.p.p.'s is also more affected by raniditine, though the kinetic behaviour observed is not a unique feature of this drug alone.

Animals↗

Cholinergic effects of cimetidine and ranitidine.

Cimetidine and ranitidine were submitted to eight in vitro assays: their intrinsic activity was evaluated on guinea-pig auricles and ileum, acetylcholine synergism on guinea-pig tracheal muscle, frog rectus abdominis, guinea-pig vas and rat phrenic nerve diaphragm, and antagonism on guinea-pig auricles and rat jejunum estimated at a range of concentrations. Ranitidine alone opposed 1-hyoscyamine antagonism in guinea-pig ileum when acetylcholine was the agonist, but not when the agonist was bethanechol.

Acetylcholine↗

[Cecal and sigmoid volvulus].

The Authors present the etio-pathogenetic, clinical and diagnostic aspects of cecal and sigmoid volvulus. They discuss the therapeutic indications and possibilities comparing advantages and disadvantages of conservative and surgical treatment. Two cases of cecal volvulus and two of sigmoid volvulus, are presented and their peculiar aspects underlined as well as the surgical technique.

Adult↗

[Cholinergic antagonism by beta-blockers. I. Spectrum of interactions].

Complete final steady state selective antagonism by beta-blockers of different conventional classes versus acetylcholine effects on isolated frog rectus abdominis, guinea pig ileum and spontaneous beating auricles had been measured. The results do not support common beta-blockers groupings, nor binary conventional subdivision of "nicotinic" and "muscarinic" cholinergic receptors, confirming our previous findings.

Abdominal Muscles↗

[Antiglaucomatous therapy with reduced concentrations (author's transl)].

By reducing the concentration of hypotensive drops and increasing the number of instillations, a therapeutic effect similar to that of the concentrated drop can be obtained, with a reduction of side-effects. The results of experiments with pilocarpine, adrenaline-guanethidine combination and propranolol are described.

Drug Therapy, Combination↗

Cholinergic compounds VII - Synthesis and pharmacological activity of some trimethylammonium iodides related to desethermuscarine.

Some substances similar to desethermuscarine were synthesized and studied as cholinergics on isolated organs. The results show the importance of the cyclopentane nucleus with regard to activity. The activity of 3-methyltrimethylammonium hexane iodide is particularly interesting for, though lacking the oxygenated function in 3 and having a different methyl spatial arrangement, this compound is only ten times less active than desethermuscarone.

Animals↗

Effects of group-selective reagents on rabbit muscle glycogen synthase.

A series of amino acid reagents was tested on the glucose-6-P dependent D, and independent I forms of glycogen synthase (UDPG: glycogen alpha-4-glucosyltransferase, EC 2.4.I. II) from rabbit skeletal muscle, at two levels of purification. Whereas blocking of aliphatic hydroxyl groups did not result in any inhibition of the enzyme(s), blocking of aromatic hydroxyl groups resulted in a gradual and complete inhibition. Under the stated assay conditions both forms of the enzyme were similarly affected in terms of activity, but the tyrosines of the D form were found to react more readily chemically. Tyrosine appears to be "essential" for catalysis. No desensitization to the allosteric modulator glucose-6-P was detected.

Affinity Labels↗

Cholinergic compounds. III - Synthesis and biological activity of epi-desmethyldesethermuscarine, desmethyldesethermuscarine and desmethyldesethermuscarone.

As a further contribution to better understanding of the nature of the cholinergic receptors, desmethyldesethermuscarone (I), epi-desmethyldesethermuscarine (II a) and desmethyldesethermuscarine (II b) were synthesized. With few exceptions, the drop in muscarinic activity of these compounds compared with that of desethermuscarone and desethermuscarines emphasizes the importance of C-7 methyl (5). As far as nicotinic activity is concerned, C-7 methyl appears much less critical.

Animals↗