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Biomedical subjects

M Guarneri

Publications and source records attributed to M Guarneri.

At least 127 records · Page 7Linked to original sources
PubMed1980

[Synthesis of compounds with antisecretory activity].

Some indole and pyrrolidone derivatives of two peptides, H-Ile-His-Pro-NH2 and N epsilon-Boc-Lys-Ile-His-Pro-NH2, were prepared and tested for antisecretory activity. A report is given of the synthetic scheme used for the two peptides which is a modified Jones procedure, the preparation of pyrrolidin-5-one-N-heptanoic acid and 1H-indol-3-heptanoic acid, the introduction on the peptide chain of indole and pyrrolidone radicals and the results of the pharmacological investigation.

Animals↗
PubMed1979

Localization of S-[methyl-14 C]adenosyl-L-methionine in pregnant mice and fetuses as determined by autoradiography.

The distribution of S-[methyl-14C]Adenosyl-L-methionine has been examined in pregnant mice using an autoradiographic technique. The results indicate that the compound crosses the placental barrier quite slowly and accumulates in some fetal tissues such as intestine, liver, kidney, eye and lung. The highest concentration is reached 12 hours after i.v. administration of the compound. In the placenta the labelling can be detected for a long time after administering the radioactive compound.

Animals↗
PubMed1979

Studies on trypsin inhibitors. Part IX. Synthesis and trypsin inhibitory activity of the duopentacontapeptide corresponding to the amino acid sequence of porcine pancreatic secretory trypsin inhibitor II (Kazal).

The synthesis of the protected duopentacontapeptide corresponding to the entire amino acid sequence I-52 of porcine pancreatic secretory trypsin inhibitor II (Kazal type) is described. The benzyloxycarbonyltetradecapeptide tert-butyloxycarbonylhydrazide (sequence 1-14) was selectively deblocked with trifluoroacetic acid and used to acylate, by the azide procedure, the peptide free base corresponding to the sequence 15-52. The isolated material was purified by ion exchange chromatography and the protecting groups were removed by successive treatments with anhydrous hydrogen fluoride, 1 M piperidine and mercuric acetate. F02M phosphate buffer, pH8. Determination of the inhibitory capacity indicated that the synthetic material is about 50% effective, at 30:1 inhibitor:trypsin molar ratio in inhibiting the tryptic hydrolysis of Nalpha-benzoyl-DL-arginine-4-nitroanilide. Full inhibition was achieved at a higher inhibitor:trypsin molar ratio. The stability constants and the standard free energy of binding of the complex between trypsin and the synthetic inhibitor have been determined.

Amino Acid Sequence↗
PubMed1979

1H nuclear-magnetic-resonance studies of the porcine-pancreatic secretory trypsin inhibitor at 270 MHz.

The pancreatic secretory trypsin inhibitor from porcine pancreas has been investigated by high-resolution 1H nuclear magnetic resonance (NMR) at 270 MHz. The presence of a number of slowly exchanging labile protons indicates that the protein is highly globular. Of the two tyrosyl rings, one is free-rotating and solvent-exposed while the other one is hindered in its mobility and buried in the interior of the protein. A lineshape analysis of the temperature dependence of aromatic resonances gave the dynamic parameters for activation of ring mobility. The inhibitor exhibits at least three well-resolved high-field ring-current-shifted methyl resonances. Form II of the inhibitor, that lacks the first four residues, has been compared with the intact form I. No detectable differences were found between the spectra of I and II, which indicates that the presence of the N-terminal tetrapeptide does not appreciably affect the overall conformation of the protein.

Animals↗
PubMed1979

Depot neuroleptics in the treatment of acute psychoses.

The data reported in the present study are derived from clinical records of 43 acute inpatients treated with the depot neuroleptic F.D. during a one year period, at the Psychiatric Institute of the University of Pisa. The criteria of selection of acute patients of schizophrenic, manic and schizoaffective type are reported. With such treatment it was possible to eliminate the stressful forced repeated drug administrations without any particular side-effects and the drug combinations were greatley reduced. However the clinical observations of this study need further confirm.

Acute Disease↗
PubMed1979

Autoradiographic distribution study of 14C-2-phenyl-6-sulfonamido-7-chloro-1,2,3,4-tetrahydro-4-quinazolinone (fenquizone) in mice.

The distribution of 2-phenyl-6-sulfonamido-7-chloro-1,2,3,4-tetrahydro-4-quinazolinone (fenquizone, M.G. 13054) labelled with 14C in mice was studied by means of an autoradiographic technique. High concentration of radioactivity was found in the intestine, liver, kidney, blood, myocardium and skeletal muscles in decreasing order at various times after oral administration. The drug was easily absorbed in the intestine reaching the highest concentration between 2 and 4 hr. The labelled compound did not cross the blood-brain barrier.

Animals↗
PubMed1978

Synthesis and prostaglandin-like activity of 2-(trans-3-hydroxy-1-octenyl)-3-indoleheptanoic acid.

The synthesis of 2-(trans-3-hydroxy-1-octenyl)-3-indoleheptanoic acid (1) is described. The title compound appeared to show a weak prostaglandin-like activity in two different systems. It contracted rat stomach fundus strips and guinea-pig ileum preparations only at concentrations about 10(3)- and 10(2)-fold higher, respectively, than PGE1. Moreover, it stimulated adenylate cyclase from rat liver plasma membrane, but the relative potency was 4--5 X 10(2)-fold lower than the natural compound. The title compound showed also a certain degree of PGE1 antagonism.

Animals↗
PubMed1978

Distribution of 14C-bis-(p-acetoxyphenyl)-cyclohexylidenemethane (F 6066) in mice.

The distribution of 14C-bis-(p-acetoxyphenyl)-cyclohexylidenemethane (14C-F 60666, cyclofenil) in mice was studied by means of an autoradiographic technique and organ radioassay. High concentration of radioactivity was found in liver, pancreas, hypophysis, lung, salivary glands, myocardium, blood, skeletal muscles and brain in decreasing order at various times after the administration. The drug penetrated very easily the blood-brain barrier and the highest concentration in the brain was detected in the hypophysis. The radiochemical studies confirm the autoradiographic data. 14C-F 6066 crossed the placental barrier and traces of radioactivity were seen in the foetuses.

Animals↗
PubMed1977

Kinetics of distribution of amphetamine in cats.

The distribution and metabolic fate of amphetamine were studied in cats. In the brain, high levels of drug were detected in the grey matter structures at short intervals after administration, while at longer intervals distribution between white and grey matter areas was more uniform. In peripheral tissues the greatest concentration of the drug was seen in the highly vascularized organs. Para-hydroxy-amphetamine was found in minimal amounts in the liver and kidneys and only at trace quantities in the brain.

Amphetamine↗
PubMed1976

[Use of oximinoiminopyrrazoline esters in the synthesis of solids phase peptides: synthesis of bradykinin].

Since oximinyliminopyrrazoline ester (OPmp) present a peculiar characteristic in the omogenous peptide synthesis, the use of them, also in the synthesis of bradikinine by the solid phase technique, was duly taken into consideration and tried out. This synthesis was achieved by employing N-protected amino acid OPmp esters containing a methoxycarbonyl or a benzylaminocarbonyl as the acyl function in position 5 of the pyrazoline ring. No significant differences were found in the reactivity of such derivatives in respect of OPmp esters containing the benzyloxycarbonylglycyl moiety. The biological activity of the synthetized braikinine is similar to that of a sample of natural "standard".

Bradykinin↗
PubMed1975

[Esters and amides of salicyloylamino acids].

N-Salicyloylamino acids, esters and amides have been prepared by the usual condensation methods and also by methods which may demonstrate 2-(o-hydroxyphenyl)oxazoline-5-ones as possible reaction intermediates. Some derivatives display pharmacological activities.

Amino Acids↗