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Biomedical subjects

E Marmo

Publications and source records attributed to E Marmo.

At least 73 records · Page 4Linked to original sources
PubMed1987

Isonicotinates, nicotinates and clofibrates of N-methyl-N-(2-hydroxyethyl or 3-hydroxypropyl)--1,3,3-trimethylbicyclo [2.2.1]heptan-2-endo-amine with hypocholesterolemic and hypolipidemic activity.

The synthesis of isonicotinic, nicotinic and clofibric esters (III a, b, c) and (IV a, b, c) starting from N-methyl-N-(2-hydroxyethyl or 3-hydroxypropyl)-1,3,3-trimethylbicyclo [2.2.1] heptan-2-endo-amine is described. In general these esters showed a normolipemic activity in rats; in particular, the isonicotinic ester (IV a) showed a hypocholesterolemic activity higher than that of clofibric acid.

Animals↗
PubMed1987

N'-acyl-N,N-(1,3,3-trimethylbicyclo [2.2.1]hept-2-ylidene)benzamidines with hypotensive activity.

The reaction of fenchone nitrimine (I) with benzamidine gave in good yield N,N-(1,3,3-trimethylbicyclo [2.2.1]hept-2-ylidene)benzamidine (II), which by acylation afforded N'-acyl-N,N-(1,3,3-trimethylbicyclo[2.2.1]hept-2-ylidene)benzam idines (III a-f) in excellent yields. Compounds (III) showed a moderate hypotensive activity in rats and a weak local anesthetic activity by infiltration in mice. Effects on heart rate and antiarrhythmic activity in rats are also reported.

Amidines↗
PubMed1987

Prenatal and postnatal antimony exposure in rats: effect on vasomotor reactivity development of pups.

Pregnant female rats were exposed to antimony trichloride (0.1 and 1 mg/dl in their drinking water ad libitum) from the first day of pregnancy until weaning (22nd day after delivery). Pups were exposed to antimony trichloride (0.1 and 1 mg/dl in their drinking water ad libitum) from 22nd until 60th day of age. Antimony exposure did not significantly affect maternal and pup systolic arterial blood pressure, length of gestation, and number of newborn per litter. Antimony exposure decreased maternal and pup body weight. No macroscopic teratogenic effects have been observed. Whether or not pups were exposed to antimony trichloride, pressor responses to carotid occlusion and 1-noradrenaline and hypotensive responses to 1-isoprenaline and acetylcholine were significantly higher on the 60th than on the 30th day of age. In pups, prenatal and postnatal antimony exposure did not affect pressor response to carotidal occlusion, while it decreased pressor response to 1-noradrenaline and hypotensive response to 1-isoprenaline on the 60th day after birth. At last, antimony exposure at higher concentration decreased pup hypotensive response to acetylcholine on the 60th day.

Animals↗
PubMed1987

Participation of GABAergic mechanisms in the hypotensive and bradycardic effects of clonidine: experimental study in conscious normotensive and hypertensive rats.

In conscious rats with normal arterial blood pressure or with spontaneous or DOC induced hypertension, effects of drugs increasing (cycloserine, ethanolamine-o-sulphate, piracetam, chlordesmethyldiazepam) or depressing (bicuculline, Ro 15-1788, PK 11195) GABAergic reactivity were evaluated on the arterial hypotension and sinus bradycardia induced by clonidine. Clonidine was administered orally by gastric gavage (0.1-1 mg/kg). Pretreatment with cycloserine, ethanolamine-o-sulphate, piracetam or chlordesmethyldiazepam increased the hypotension and sinus bradycardia induced by clonidine. On the contrary, pretreatment with bicuculline or Ro 15-1788 reduced the cardiovascular effects of clonidine. These results suggest that the GABAergic system is involved in cardiovascular effects of clonidine in normotensive and hypertensive rats.

Animals↗
PubMed1987

Central and peripheral cardiovascular effects of beta-endorphin in normotensive and spontaneously hypertensive rats and in rats rendered hypertensive by deoxycorticosterone acetate administration.

The cardiovascular effects of beta-endorphin [beta-LPH-(61-91)] were investigated after systemic (i.v.) and central (third ventricle and right lateral ventricle) administration in urethane-anesthetized rats. beta-Endorphin (10 and 100 micrograms/kg i.v. or 40 micrograms into the third ventricle or into the lateral ventricle) in normotensive animals induced a decrease in blood pressure and bradycardia. The same dose of beta-endorphin by systemic and central administration induced much more pronounced cardiovascular effects in spontaneously hypertensive rats and in rats rendered hypertensive by DOCA administration than in normotensive rats. Naloxone i.v. pretreatment reduced the cardiovascular effects induced by beta-endorphin.

Animals↗
PubMed1987

N-acyl-N'-methyl-N-(1,3,3-trimethylbicyclo[2.2.1]hept-2-yl) benzamidines with hypotensive activity.

Lithium aluminium hydride reduction of N-phenoxycarbonyl-N,N-(1,3,3-trimethylbicyclo[2.2.1]-hept-2- yl)benzamidine (II), which afforded the N-acyl derivatives (III a-f) in good yields. Compounds (II) and (III) showed a moderate hypotensive activity in rats. Local anesthetic activity by infiltration in mice, effects on heart rate and antiarrhythmic activity in rats are also reported.

Amidines↗
PubMed1987

Esters of N-(2-hydroxy-1,1-dimethylethyl)-1,7,7-trimethylbicyclo[2.2.1] heptan-2-exo-amine with hypotensive activity.

The synthesis of title compounds by reaction of camphor nitrimine with 2-amino-2-methylpropanol, followed by NaBH4 reduction of the resulting imine to the aminoalcohol (III) and esterification of (III) with aliphatic and aromatic acyl chlorides in pyridine solution, is described. Phenyl carbamate (V) was also prepared by reaction of (III) with phenyl isocyanate. Some esters and (V) showed a moderate hypotensive activity in rats. Effects on heart rate and antiarrhythmic activity in rats, as well as infiltration anesthesia in mice, are also reported.

Amines↗
PubMed1987

Research on heterocyclic compounds. XXII. Imidazo[1,2-a]pyrimidines.

We have taken into consideration a group of 21 imidazo [1,2-a]pyrimidine derivatives, some of which were already known, whereas the others were synthesized and characterized by us to complete the series. Antiinflammatory, analgesic, antipyretic and ulcerogenic activities of such compounds were evaluated in comparison with indomethacin, in order to get useful information about structure-activity relationships.

Animals↗
PubMed1987

Respiratory responses to pirenzepine in healthy subjects.

Since no information is available concerning the action of pirenzepine in vivo on human tracheobronchial tree, we evaluated the respiratory responses to pirenzepine in a group of healthy subjects. This clinical study suggests that pirenzepine exerts its bronchodilatory action on small airways (from 9th generation to distal airways), but not on larger airways, in normal subjects. These results are consistent with a probable presence of muscarinic high affinity receptors (M1 subtype) only in peripheral airways.

Adolescent↗
PubMed1987

Esters of N-methyl-N-(2-hydroxyethyl or 3-hydroxypropyl)-1,3,3-trimethylbicyclo [2.2.1]heptan-2-endo-amine with hypotensive activity.

The synthesis of title compounds by reaction of fenchone nitrimine with 2-aminoethanol and 3-aminopropanol, followed by stereospecific NaBH4 reduction of the resulting imines, Eschweiler-Clarke reductive methylation and esterification with aliphatic and aromatic acyl chlorides is described. Some esters showed an appreciable hypotensive activity in rats. Effects on heart rate and antiarrhythmic activity in rats, as well as infiltration anesthesia in mice, are also reported.

Anesthetics, Local↗
PubMed1987

Benzamides and cholinesterases.

At certain doses metoclopramide (MT), sulpiride and bromopride produce anti-cholinesterase effects as shown by studies on the serum and erythrocyte cholinesterases of the rabbit and the dog, and by those on the hypotensive effect of ACh incubated with rabbit serum in the presence or absence of MT. The anti-cholinesterase effect of MT was more intensive than that of sulpiride, bromopride, procainamide or procaine, but less pronounced than that of prostigmine.

Acetylcholine↗
PubMed1986

Central antiarrhythmic effects of imidazole in anesthetized rats.

In urethane anesthetized rats, the intracerebroventricular (icv.) microinjection of sodium glutamate or KCl induced cardiac arrhythmias. These cardiac rhythm disorders could be prevented by the icv. administration of imidazole. The i.v. injection of the same doses of imidazole elicited cardiac arrhythmias. The antiarrhythmic activity of imidazole is probably due to its ability to stimulate phosphodiesterase activity, which leads to a decrease in cGMP and/or cAMP cerebral levels.

Anesthesia↗
PubMed1986

Aminoethers of (+)-1,3,3-trimethyl-2-oxabicyclo[2.2.2]-octan-6-hydroxyimine with hypotensive activity. II.

The synthesis of a series of N-substituted 3-amino-2-hydroxypropyl ethers (III a-1) starting from (+)-1,3,3-trimethyl-2-oxabicyclo [2.2.2]-octan-6-hydroxyimine is described. Some of these compounds showed a remarkable hypotensive and a weak bradycardic activity in rats, as well as a moderate local anesthetic activity in mice. All compounds were found to be devoid of antiarrhythmic activity in rats and of beta-blocking activity in dogs.

Adrenergic beta-Antagonists↗
PubMed1986

Effect of Salmonella typhimurium porins on the cardiovascular and renal apparatus.

The cardiovascular effects of porins were evaluated using porins isolated from Salmonella typhimurium SH5014. In dogs porins depress arterial systemic pressure, vasomotor reactivity of norepinephrine and peripheral vagal stimulation. They are capable of modifying the sinocarotidal baroreceptor reactivity. In mice porins increase the cardiotoxic effects of isoprenaline, thyroxine, emetine and of p-nitrophenol. In rats porins increase the arrhythmogenic and lethal effects of BaCl2 and also give rise to renal lesions, probably at the tubular level.

Animals↗
PubMed1986

Research on heterocyclic compounds. XIX--2-Methylimidazo[1,2-a]pyridine-3-acetic acids.

A group of methyl substituted imidazo[1,2-a]pyridine-3-acetic acids was synthesized by reaction of some methyl derivatives of 2-aminopyridine with ethyl 3-bromolevulinate and subsequent hydrolysis. These new acidic compounds were tested for their antiinflammatory, analgesic, antipyretic and ulcerogenic activities in order to compare the results with those previously obtained with similar compounds.

Animals↗