Biomedical subjects
Publications and source records attributed to E Marmo.
In vitro researches documented that reproterol, as well as salbutamol, is a powerful stimulant of adenyl cyclase activity in the trachea and bronchi but less potent than isoprenaline. The stimulation was antagonized by beta-blockers.
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The effects of 15(S) 15-methyl-PGF2 alpha were studied on the cardiovascular system of dogs. Intravenous and intravertebral artery administration of 15(S)-methyl-PGF 2 alpha induced arterial hypertensive and respiratory effects more intense and longer lasting than those observed for PGF2 alpha. Intravenous administration of 15(S) 15-methyl-PGF2 alpha induced a decrease of vascular reactivity to 1-norepinephrine and 1-epinephrine and to carotidal occlusion. Infiltration of the carotid sinus walls with 15(S) 15-methyl-PGF2 alpha decreased the baroreceptor reactivity.
Fructose-1,6-diphosphate (FDP) has been reported to exert beneficial effects on several cardiac functions. We studied the effects of FDP on the biochemical and dynamic functions of the heart in anesthetized dogs. Significant effects of FDP were noted mostly as related to pyruvate and lactate metabolism. The results seem to indicate that FDP may improve heart metabolism, and coronary function in restricted animals.
The synthesis of a series of 2-methylimidazo[1,2-a]pyridine-3-carboxylic acids was accomplished by reacting some 2-aminopyridines with ethyl 2-chloroacetoacetate and then hydrolyzing the resulting ethyl carboxylates. Such new carboxylic acids were evaluated for antiinflammatory, analgesic, antipyretic, and ulcerogenic activities.
The synthesis of N-substituted 1,7,7-trimethyl-2-piperidinobicyclo[2.2.1]hept-2-ene 3 carboxamides (II) by reaction of 1,7,7-trimethyl-2-piperidinobicyclo[2.2.1]hept-2-ene (I) with alkyl and aryl isocyanates, as well as the alkaline hydrolysis of (II) to N-substituted 1,7,7-trimethylbicyclo[2.2.1]heptan-2-one 3 carboxamides (III), are described. A number of compounds (II) and (III) showed strong hypotensive and bradycardiac activities in rats, as well as weak infiltration anesthesia and antiarrhythmic activity in mice. Antiacetylcholine activity in vitro is also reported.
Experimental investigations have shown that inosine enhances purinergic reactivity. This was examined with adenosine at the level of the cardiovascular, intestinal and uterine musculature. The mechanism of this activity may probably be inhibition of uptake without significantly altering serum adenosinase.
The synthesis of ureas (IV) and amides (V) derived from the tricyclic terpenoid amine 5,7,7-trimethyl-6-oxa-3-azatricyclo[3.2.2.0(2.4)]nonane (III) is described. A number of these compounds showed hypotensive and bradycardic activity in rats, as well as infiltration anesthesia and antiarrhythmic activity in mice. In particular, the n-butylurea (IV b) was superior to lidocaine concerning the anesthetic effect, and the benzamide (V f) showed the same degree of local anesthetic and antiarrhythmic activity as lidocaine. Antiacetylcholine activity in vitro and antitumor activity against P388 lymphocytic leukemia in mice are also reported.
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In vitro in vivo reproterol showed intense spasmolytic effects upon the trachea and bronchi against various spasm-including agents (histamine, acetylcholine, acetyl-beta-methylcholine, 5-hydroxytryptamine, BaCl2). A comparative study with various drug used in the treatment of asthma (isoprenaline, metaproterenol, salbutamol, clenbuterol, papaverine and atropine) has been conducted.
A series of aliphatic and aromatic esters of 1,7,7-trimethyl-2-exo-piperidinobicyclo[2.2.1]heptan-3-endo-ol is described. A number of these compounds showed antiarrhythmic activity in guinea pigs and mice, as well as surface anesthesia in rabbits and infiltration anesthesia in mice. Circulatory, cardiac and respiratory effects in dogs are also described.
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In rats with cannulae chronically implanted into specific areas of the brain, the effects of beta-endorphin were studied on behavior and electrocortical activity. It has been shown that analgesia and catatonia were evoked after infusing beta-endorphin into the III cerebral ventricle or into the hypothalamus. On the contrary, beta-endorphin microinjected into the caudate nucleus or into the substantia nigra produced an intense pattern of stereotyped movements, occasional contralateral circling, contralateral myoclonic jerks and asymmetric posture. Stereotyped gnawing, grooming and "wet-dog" syndrome preceded catatonia after intrahypothalamic administration of beta-endorphin. Bilateral (III ventricle) or ipsilateral (hypothalamus, caudate nucleus and substantia nigra) high voltage electrocortical spikes and other ECoG pathological changes accompanied by motor disorders (stereotypies, myoclonic jerks) or without any overt behavioral change were constantly observed. Behavioral and electrocortical changes evoked by beta-endorphin were long-lasting and rapidly reversed by the specific opiate antagonist, naloxone.
Since we had previously observed the considerable anti-inflammatory activity of imidazo[1,2-a]pyrazine 2-acetic acid, we prepared a series of imidazo[1,2-a]pyrazine derivatives, bearing some substituents on the pyrazine ring and a carboxylic, acetic or alpha-methylacetic moiety on the imidazole ring. These new compounds were tested for antiinflammatory, analgesic, antipyretic and ulcerogenic activities.
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