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Biomedical subjects

E Marmo

Publications and source records attributed to E Marmo.

At least 91 records · Page 5Linked to original sources
PubMed1986

Derivatives of 1,2,3,3-tetramethyl-2-azabicyclo-[2.2.2]octan-5-trans-ol with antiarrhythmic and other activities. VI.

The synthesis of a series of alkyl and aryl amides (IV) starting from 5-trans-(3-aminopropoxy)-N-benzyl-1,2,3,3-tetramethyl-2-azabicyclo [2.2.2] octane is described. Some of compounds (IV) showed a moderate hypotensive activity in rats and infiltration anesthesia in mice. Effects on heart rate in rats and antiarrhythmic activity in mice were practically absent.

Anesthetics, Local↗
PubMed1986

1,3,3-Trimethyl-N-(2-pyridyl)-2-oxabicyclo[2.2.2]octan-6-amine derivatives with hypotensive and other activities.

The synthesis of 1,3,3-trimethyl-N-(2-pyridyl)-2-oxabicyclo-[2.2.2]octan-6-amine (cis, trans mixture) starting from 1,3,3-trimethyl-N-nitro-2-oxabicyclo[2.2.2]octan-6-imine, as well as of a series of amides (V) derived from the above amine, is described. Some compounds (V) showed strong hypotensive activity in rats. Effects on heart rate and antiarrhythmic activity in rats, as well as local anesthetic activity in mice, are also reported.

Anesthetics, Local↗
PubMed1986

Behavioral and electrocortical effects of tolonidine in rats.

The rats systemic administration of tolonidine in rats (0.05-5.0 mumol/Kg) produced behavioural and electrocortical slow-wave sleep lasting between 35 and 200 min depending on the dose. In addition, a dose-dependent fall in deep body temperature was observed. Similar effects were evoked by infusing tolonidine (5-80 nmol) into the third cerebral ventricle. Behavioural, ECoG and body temperature effects were prevented by previous intraventricular or systemic injection of phentolamine, an antagonist at alpha 1- and alpha 2-adrenoceptors, and of yohimbine, an antagonist at alpha 2-adrenoceptors, whereas prazosin, an alpha 1-adrenoceptor antagonist, was ineffective. In conclusion, the present experiments show that tolonidine possesses central effects similar to those evoked by clonidine and provide further evidence in favour of the idea that central alpha 2-adrenoceptors are involved in the control of slow-wave sleep and body temperature.

Animals↗
PubMed1986

Central antiarrhythmic activity of adenosine in anesthetized rats.

In urethane-anesthetized rats the intracerebroventricular (icv.) administration of sodium glutamate or desipramine induced cardiac arrhythmias. These cardiac rhythm disturbances could be prevented by icv. administration of adenosine. The i.v. injection of adenosine had an arrhythmogenic action. The antiarrhythmic effect of adenosine could be reversed by icv. aminophylline. It is suggested that the antiarrhythmic activity of adenosine is due to the central inhibition of release of acetylcholine, and/or noradrenalin, produced by the decreased availability of calcium for the excitation-secretion coupling.

Adenosine↗
PubMed1986

On the mechanism of the anti-hypertensive effect of Ca++-blockers.

Cardiovascular effects induced by nifedipine and verapamil were examined in normo- and hypertensive animals to investigate the role of Ca++ -antagonists in antihypertensive therapy. Intra-arterial administration of nifedipine or of verapamil to anesthetized dogs by the intracerebroventricular (icv, 1 and 10 micrograms/kg in 1 min), or intravertebral (0.1 and 1 mg/kg in 5 sec) or intra common carotid artery (0.1 and 1 mg/kg in 5 sec) produced hypotension and sinus bradycardia and slightly reduced the pressor response induced by carotid occlusion. The latter effect was also reduced when the drugs were infiltrated into the walls of carotid sinuses (0.1 ml/sinus of a 1% solution). The antihypertensive effect of nifedipine and verapamil depends on their Ca++ antagonist and vasodilator properties. However, our study suggests CNS vasomotor involvement also.

Anesthesia↗
PubMed1985

Research on heterocyclic compounds. XVIII. Imidazo[2,1-b]-1,3,4-thiadiazole derivatives.

The synthesis of a series of 6-carbethoxy-, 6-carbethoxy-methyl-, and 5-carbethoxy-6-methylimidazo[2,1-b]-1,3,4-thiadiazoles was accomplished by reacting some 2-amino-1,3,4-thiadiazoles with ethyl bromopyruvate, 4-chloroacetoacetate, and 2-chloroacetoacetate, respectively; such carbethoxy derivatives afforded the corresponding carboxylic acids by hydrolysis. The antiinflammatory, analgesic, antipyretic and ulcerogenic activities were studied on three of the new acidic compounds.

Animals↗
PubMed1985

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

The synthesis of beta-dialkylaminoethyl ethers (II a-f) and gamma-dialkylaminopropyl ethers (II g-i), as well as of aryl carbamates (III 1, m), starting from (+)-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-hydroxyimine (I), is described. beta-Dimethylaminoethyl ether (II a) showed a remarkable hypotensive and bradycardic activity in rats; moreover, nearly all compounds (II) and (III) exhibited a weak antiarrhythmic activity in rats. Infiltration anesthesia in mice, beta-blocking activity in dogs and antiacetylcholine activity in vitro are also reported.

Acetylcholine↗
PubMed1985

Cardiovascular effects of tetanus toxin after systemic and intraventricular administration in rats.

A single intraperitoneal injection of tetanus toxin (50,100 and 200 minimum lethal dose per rat) produced a significant and dose-dependent increase in systemic blood pressure and heart rate in conscious rats. On the contrary, tetanus toxin, given directly into the third cerebral ventricle (20 and 40 minimum lethal dose), produced a gradual and dose-dependent decrease in blood pressure accompanied by bradycardia. In conclusion, the present findings show that tetanus toxin is able to affect cardiovascular activity and it is suggested that this may be due to an interference with central GABAergic mechanisms.

Animals↗
PubMed1985

Pharmacological properties of a new non-steroidal anti-inflammatory drug: flunoxaprofen.

The anti-inflammatory, analgesic and antipyretic activities of S-(+)-2(4-fluorophenyl)-alpha-methyl-5 benzoxazole acetic acid (flunoxaprofen: Flu), a new non-steroidal anti-inflammatory drug, were compared with those of indomethacin and other non-steroidal anti-inflammatory drugs (NSAIDs) in experimental animals. Flu showed strong inhibitory activity on acute and subacute inflammation tests in rats, such as carrageenin hind paw oedema (oral: 6-25 mg/kg; rectal: 50-100 mg/kg); pellet-induced granuloma formation (5-20 mg/kg/day) and adjuvant-induced arthritis (10 mg/kg/day). Its potency was comparable with that of indomethacin (I) and higher than that of acetyl salicylic acid (ASA), ibuprofen (IBU) or phenylbutazone (P). The analgesic activity of Flu, evaluated by the hot plate method and tail pinching in mice, was slightly lower than that of I but higher than that of ASA and IBU. In pyretic rabbits Flu showed an antipyretic activity higher than that of ASA and IBU. The ability of Flu to affect platelet aggregation, mucopolysaccharide synthesis by fibroblasts and the proteolytic action of trypsin was also investigated.

Animals↗
PubMed1985

Organ tolerance of non-steroidal anti-inflammatory drugs: effect on liver cells.

Experimental studies in mice and in rats showed the good tolerance of a new non-steroidal anti-inflammatory drug, flunoxaprofen, by normal and CCl4 damaged liver. The activity of an enzyme-inducing drug, such as phenobarbital, showed a greater increase after pretreatment with indomethacin than with flunoxaprofen or benoxaprofen. High doses of benoxaprofen and indomethacin significantly decreased bromosulphonphthalein excretion in rats with normal or CCl4 damaged liver; the effect was not observed with flunoxaprofen administered at the same dose as benoxaprofen. Moreover, benoxaprofen and indomethacin but not flunoxaprofen induced a significant increase of some serum liver enzymes in CCl4 poisoned rats.

Animals↗
PubMed1985

2-Substituted-3-pyridinolethers as hypolipidemic and platelet aggregation inhibiting agents.

Some 2-substituted 3-pyridinolethers were synthesized, with one side chain bearing a carboxylic function; among these there are products having structure analogies with the prostaglandins. The results of hypolipidemic and hypocholesterolemic tests on experimental hyperdyslipidemic animals, as well as those on the inhibition of platelets aggregation and on fibrinolytic activity are reported.

Animals↗
PubMed1985

N-substituted 4,7,7-trimethyl-3-(1-piperidinyl)bicyclo-[2.2.1]hept-2-ene 2-carboxamides and 2-carbothioamides with hypotensive activity.

The synthesis of two series of N-substituted 4,7,7-trimethyl-3-(1-piperidinyl)bicyclo[2.2.1]hept-2-ene 2-carboxamides (I d-h) and 2-carbothioamides (I i-o), as well as of some N-aryl 4,7,7-trimethyl-3-(1-pyrrolidinyl)bicyclo[2.2.1]hept-2-ene 2-carboxamides (I a-c), by reaction of camphor piperidinoenamine and pyrrolidinoenamine with aryl isocyanates and isothiocyanates is described. On the whole compounds (I d-h) showed a weak hypotensive activity in rats.

Animals↗