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Biomedical subjects

R Gaggi

Publications and source records attributed to R Gaggi.

At least 55 records · Page 3Linked to original sources

[Preparation and analgesic activity of tetrahydroquinolines and tetrahydroisoquinolines].

A series of 1,2,3,4-tetrahydroquinolines and of 1,2,3,4-tetrahydroisoquinolines were synthesised and evaluated for analgesic activity by both hot-plate and acetic acid writhing methods in rats. Te most potent compound was 2-methyl-1,2,3,4-tetrahydro-5-quinolinol (IV i) which was shown to be 1/8 and 1/50 as active as morphine according to the employed assay. The analgesic activity was shown to be associated to a not selective action on the CNS.

Analgesics↗

Involutional dementias: new perspectives.

13 patients with psycho-organic syndrome (POS) and 10 patients with dementia (senile, Alzheimer, multi-infarct) were treated with drugs considered to influence the neuronal turnover of acetylcholine (Phosphatidylcholine, piracetam, S-adenosylmethionine) for 30 days and compared in respect of CSF ACh levels, reaction times to simple visual stimuli (TRS-V) and to simple hearing stimuli (TRS-H) and scores on the Sandoz Clinical Assessment Geriatric (SCAG) rating scale. The POS patients presented higher CSF ACh levels, shorter TRS-V and TRS-H times and lower SCAG scores than the demented patients before treatment. During treatment the CSF ACh values fell in the POS but not in the demented patients. All the other values improved in both groups but more markedly in the POS group. The CSF ACh variations in the latter appear to correlate with the variations in TRS-V and TRS-H times and SCAG scores. The monitoring of CSF ACh would seem to be useful in assessing both the degree of decline in dementia and the possibilities of treatment in individual patients.

Aged↗

Relationships between hypocalcaemic and anorectic effect of calcitonin in the rat.

Salmon calcitonin (sCT, 2 and 20 U/kg), porcine calcitonin (pCT, 20 and 40 U/kg) and human calcitonin (hCT, 20 and 40 U/kg) were injected subcutaneously to rats trained to eat their food during two hours each day. Food intake and serum Ca++ concentrations were determined at the end of 2h-feeding period. A long lasting anorectic effect was observed for 20 U/kg of sCT with a parallelism between hypocalcaemia and anorexia in the first 8 hours after treatment; on the contrary, rats continued to eat less than controls in the following hours when their serum Ca++ concentrations had risen to normal or even higher levels. As regards pCT and hCT, it was shown that these peptides reduced significantly meal size only for 1-2 hours when serum Ca++ levels were at their lowest levels for these peptides.

Animals↗

Plasma noradrenaline and blood pressure in uremia.

To evaluate a possible correlation between sympathetic activity and blood pressure in uremia, catecholamines and blood pressure were determined in 81 uremic patients. In 34 of these 81 patients, thyroid hormones were also measured. In 16 patients on maintenance dialysis, a longitudinal study was performed to compare long-term blood pressure and catecholamine variations. No correlation was found between mean blood pressure and noradrenaline in the 81 patients as a whole, but when male and female patients were evaluated separately, a significant correlation was found in the former group. In the 34 patients, a correlation between mean blood pressure and noradrenaline was found only when hypothyroid patients were excluded. Variations in mean blood pressure induced by chronic dialysis were related to noradrenaline changes in the 16 patients studied. In conclusion, sympathetic activity seems to be correlated to blood pressure in uremic patients.

Adolescent↗

Antidepressant versus neuroleptic activities of sulpiride isomers on four animal models of depression.

The atypical neuroleptic sulpiride is also prescribed for depression because of its activating effect. However, such an effect does not necessarily imply an action identical to that of classical antidepressants, and a laboratory comparison of the neuroleptic and antidepressant activities of sulpiride may contribute to a better definition of its psychotherapeutic profile. Sulpiride isomers were studied in the rat in four behavioural models of depression which are thought to be influenced by neuroleptics in different ways. Desipramine (imipramine) and haloperidol were employed in each test as a standard antidepressant and neuroleptic, respectively. The four tests were: 1) prevention of apomorphine-induced sedation: 2) antagonism of apomorphine-induced hypothermia; 3) behavioural despair (swim test); 4) learned helplessness ( FR2 lever pressing escape). Desipramine ameliorated behaviour in all tests; haloperidol ameliorated the response to test 1, influenced that to test 2 in a neuroleptic-like way and worsened the responses to tests 3 and 4. (-)-Sulpiride worked in a similar way to haloperidol in all tests. (+)-Sulpiride significantly and dose-dependently ameliorated the responses to test 3 and was inactive in the others. No conclusion was drawn from test 1 owing to its lack of specificity; the results of the remaining tests indicated a neuroleptic profile of (-)-sulpiride and suggested a potential "antidepressant" activity of (+)-sulpiride which merits further investigation.

Animals↗

[Naphthofuran derivatives with potential beta-adrenolytic activity].

1-(Naphtho[1,2-b]furan-2-yl)-2-(isopropylamino)ethanol (II) and 1-(naphtho[2,3-b]furan-2-yl)-2-(isopropylamino)ethanol (III) show low beta-adrenergic blocking activity and unlike the naphtho [2,1-b]furan derivatives (1,2) do not appear to give rise to metabolites with high beta-adrenoceptor inhibitory properties. The inclusion of the --OCH2-- moiety in an aromatic nucleus larger than the benzofuran system (bufuralol, Ro 3-3528) caused loss of the biological activity.

Adrenergic beta-Antagonists↗

Dialysable and non-dialysable hydroxyproline in the rat's urine: age related and diurnal variations.

1. Urinary dialysable and non-dialysable hydroxyproline, which are considered good indices of bone resorption and neoformation respectively, were determined in rats under conditions that modify skeleton metabolism, such as body growth and parathyroid or calcitonin administration. It was also investigated whether dialysable and non-dialysable hydroxyproline excretions showed significant circadian fluctuations in rats of different ages.2. Dialysable hydroxyproline excretion sharply decreased from the first to the fifth months of age and underwent further gradual reduction up to the fourteenth month of life. Non-dialysable hydroxyproline excretion followed a smoother decrease up to the fifth month, then remained constant. Urinary excretion of non-dialysable hydroxyproline expressed as a percentage of the total hydroxyprolinuria (n.d.%) slowly increased with advancing rat age.3. In 2-, 4- and 6-month old rats, dialysable hydroxyproline excretion showed significant circadian fluctuations with minima and maxima at the end of the dark and light fraction of the cycle respectively. Daily fluctuations were greater in young and adult rats (50-65% of the respective average levels) than in 4-month old rats (25%). Non-dialysable hydroxyproline excretion followed similar but less pronounced patterns. Significant circadian fluctuations of n.d.% were detectable only in 2- and 4-month old rats, with peaks at 04.00-05.00 hr, thus indicating that the bone formation/resorption ratio increased in the nocturnal fraction of the cycle.4. Young rats administered with calcitonin exhibited reduced levels of urinary dialysable but not of non-dialysable hydroxyproline when the hormone was given at 13.30 hr. No changes were observed when calcitonin was injected at 19.30 hr. On the contrary, both diurnal and nocturnal parathyroid hormone administration to young rats caused increased levels of dialysable and non-dialysable hydroxyproline of the same magnitude.

Age Factors↗

Experimental study on the anabolic and androgenic/antiandrogenic activity of different dose levels of medroxyprogesterone acetate (MAP) in rats.

The authors treated three groups of rats with medroxyprogesterone acetate (MAP) at different dosages (0, 2.5, 5, 10, 20, 40, 80 mg/kg) i.p. and orally for 7 days to evaluate its anabolic and its androgenic/antiandrogenic effect. 70 rats had been previously castrated and 35 were intact. The anabolic effect is evident in all groups of animals which were treated. The androgenic action predominates in castrated animals, while the antiandrogenic action predominates in intact animals. The above-mentioned actions are more marked when very high doses are used. After suggesting the possible mechanism of action of MAP, the authors point out that the anabolic effect confirms what has already been reported in clinical oncology after treatment with very high doses of MAP (1,000-2,000 mg orally or i.m. for 30 days) in different types of tumors (breast, kidney, prostate).

Administration, Oral↗

[Preparation and beta adrenolytic activity of some derivatives of naphthol-[2,1-b]furan].

Some 1-(naphtho[2,1-b]furan-2-yl)-2-(t-butylamino)ethanols were synthesized for possible beta-adrenergic receptor blockade. The compounds may be considered to be derived from naphthyloxypropanolamines, the side chain of which is partially included in a furan ring. The pharmacological profile of 1-(naphtho[2,1-b]furan-2-yl)-2-(t-butylamine)ethanol (I b) is quite similar to that of propranolol without cardiac depressant properties.

Adrenergic beta-Antagonists↗

[Effect on lipidemia in the rat of bis-homoanalogs of adenine nucleosides].

The hypolipidemic activity of a series of adenine nucleosides bis-homoanalogues was evaluated in the rat and compared with that of the sodium salt of erythadenine, used as reference standard. Some compounds were more effective in lowering serum cholesterol than erythadenine, but all showed a reduced effect on serum triglyceride content.

Adenine Nucleotides↗