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Your search keyword '"Perlini, V."' showing total 10 results
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10 results on '"Perlini, V."'

1. Synthesis of 2-Amino-5-sulfanyl-1,3,4-thiadiazole Derivatives and Evaluation of Their Antidepressant and Anxiolytic Activity

Author

Clerici, F., Pocar, D., Guido, M., Loche, A., Perlini, V., and Brufani, M.

Abstract

Recently a series of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives bearing different substituents were synthesized and screened pharmacologically in order to evaluate their central nervous system activity. The purpose of this study was to evaluate the effects of the title compounds on CNS activity by varying the substituents in the thiadiazole moiety. It was found that some of these compounds possess marked antidepressant and anxiolytic properties comparable in efficiency to the reference drugs Imipramine and Diazepam. The most potent compound 3k was further investigated to complete its pharmacological profile with respect to undesired side effects. Behavioral results showed that 3k is a very promising compound, characterized by a mixed antidepressant-anxiolytic activity accompanied by a therapeutic dose range that is essentially 2 orders of magnitude less than that at which side effects such as sedation and amnesia are evident.

Published
2001

8. Synthesis and dopaminergic activity of trans-6-methyl-7a,8,9,10,11,11a-hexahydro-7H-pyrrolo[3,2,1-gh]- 4,7-phenanthroline and trans-1,2,3,4,4a,5,6,10b-octahydro-4,7-phenanthroline derivatives.

Author

Claudi F, Cristalli G, Martelli S, Perlini V, Massi M, and Venturi F

Subjects
Animals, Bromocriptine pharmacology, Ergolines pharmacology, Male, Phenanthrolines pharmacology, Prolactin blood, Pyrroles pharmacology, Rats, Structure-Activity Relationship, Ergolines chemical synthesis, Phenanthrolines chemical synthesis, Pyrroles chemical synthesis, Receptors, Dopamine drug effects
Abstract

The synthesis and dopamine agonist activity of some derivatives of trans-6-methyl-7a,8,9,10,11,11a-hexahydro-7H-pyrrolo[3,2,1-gh]- 4,7-phenanthroline (6a-c) are reported. These compounds can be regarded as analogues of ergoline derivatives with the indole nucleus replaced by indolizine. These congeners have been evaluated as inhibitors of prolactin release in vivo. trans-6-Methyl-8-ethyl-7a,8,9,10,11,11a-hexahydro-7H-pyrrolo[3,2,1-gh]- 4,7-phenanthroline (6b) proved to produce a dose-dependent inhibition of serum prolactin that was almost complete at the highest dose employed. Although effective, this compound was far less potent than bromocriptine. The 8-propyl derivative 6c was weakly active only at very high doses, and the 8-methyl derivative 6a proved to be completely ineffective. trans-4-Propyl-1,2,3,4,4a,5,6,10b-octahydro-4,7-phenanthroline (7), a molecular simplification of hexahydropyrrolo-4,7-phenanthroline, proved to be the most potent among the newly synthesized compounds. These results, taken together with those of previous studies, suggest that the presence of the nitrogen of the indolizine nucleus and the N-7 in the octahydro-4,7-phenanthroline 7 are significant for the interaction with the dopamine receptor involved in the control of prolactin release.

Published
1986
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9. Synthesis and dopamine receptors binding affinity of 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N-alkyl derivatives.

Author

Cardellini M, Cingolani GM, Claudi F, Perlini V, Balduini W, and Cattabeni F

Subjects
Animals, Antipsychotic Agents pharmacology, Benzazepines pharmacology, Chemical Phenomena, Chemistry, Corpus Striatum drug effects, Corpus Striatum metabolism, Dopamine chemical synthesis, Dopamine metabolism, Dopamine pharmacology, In Vitro Techniques, Radioligand Assay, Rats, Receptors, Dopamine metabolism, Spiperone pharmacology, Dopamine analogs & derivatives, Receptors, Dopamine drug effects
Abstract

The 2-(3-fluoro-4-hydroxyphenyl)ethylamine and its N,N-dialkyl derivatives were synthesized. The affinity of new compounds for dopamine binding sites was measured in a test involving displacement of [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) from homogenized rat striatal tissue. No compound proved effective in displacing [3H]SCH 23390. Two derivatives are selective displacers of [3H]spiperone.

Published
1988

10. Interaction of some 2-hydroxybenzylpiperidines with dopamine receptors.

Author

Cardellini M, Claudi F, Perlini V, Balduini W, Cattabeni F, and Cimino M

Subjects
Adenylyl Cyclase Inhibitors, Animals, Benzyl Compounds chemical synthesis, Benzyl Compounds pharmacology, Binding, Competitive drug effects, Chemical Phenomena, Chemistry, Corpus Striatum metabolism, In Vitro Techniques, Male, Piperidines chemical synthesis, Rats, Rats, Inbred Strains, Spiperone metabolism, Synaptosomes enzymology, Piperidines pharmacology, Receptors, Dopamine drug effects
Abstract

Some N-alkyl derivatives of 2-(3-hydroxybenzyl)piperidine and of 2-(3,4-dihydroxybezyl)piperidine were synthesized and evaluated pharmacologically in vitro by competition with [3H]spiperone for binding to a homogenized rat striatal tissue, and for ability to stimulate adenylate cyclase. The N-methyl-2-(3,4-dihydroxybenzyl)piperidine shows a fairly good affinity for the D-2 dopamine receptor. The N-alkyl 2-(3,4-dihydroxybenzyl)piperidines produce a faible stimulation of adenylate cyclase activity.

Published
1987

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