A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its γ-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.

Furoxan

10.1021/jm020969t

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Citations (100)

Stereoselective Inhibition of Ethanol- Induced Gastric Lesions in the Rat by the H<sub>3</sub>-Receptor Agonist (R)-α-Methylhistamine and Its (S)-Configured Isomer

Pharmacology (1999)

Giuseppina Morini Daniela Grandi G. Bertaccini Christian Leschke Walter Schunack

The histamine H(3) receptor shows high degree of stereoselectivity for histamine analogues branched in the side chain. The hypothesis that gastroprotection by (R)-alpha-methylhistamine could be H(3) receptor-mediated was tested by comparing the effect of (R)-alpha-methylhistamine and of (S)-alpha-methylhistamine on ethanol-induced histologic lesions in the rat gastric mucosa. Extensive damage was caused by 60 min exposure to absolute ethanol, 91% of the mucosa examined being damaged. Conversely only 23% of the mucosa was damaged after pretreatment with (R)-alpha-methylhistamine (100 mg/kg i.g.). In the groups pretreated with (S)-alpha-methylhistamine (55.44 and 166.3 mg/kg i.g.) total damage ranged from 77 to 79%, though it was confined to the upper portion of the mucosa. Morphometric analysis of stained intraepithelial mucosubstances revealed that (R)-alpha-methylhistamine pretreatment resulted in an increase in number and volume of surface mucous cells, not evident after (S)-alpha-methylhistamine pretreatment. Scanning electron microscopy confirmed light microscopy evaluations. The two isomers of alpha-methylhistamine differently affect the response of rat gastric mucosa to absolute ethanol and they appear to differ in their influence on surface mucous cells. A basis for interpreting the effects of the two isomers of alpha-methylhistamine rests on the high degree of stereoselectivity of H(3) receptors and on the different affinities of the two isomers for these receptors.

Alpha (finance)

10.1159/000028320

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Citations (9)

The gastric effects of UFP-112, a new nociceptin/orphanin receptor agonist, in physiological and pathological conditions

Peptides (2007)

Maria Broccardo Remo Guerrini Giuseppina Morini Carlo Polidori S. Agostini

Nociceptin receptor

NOP

10.1016/j.peptides.2007.07.021

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Citations (16)

Influence of (R)-alpha-methylhistamine on the histamine H3 receptor in the rat gastrointestinal tract.

Inflammation Research (2007)

Paul L. Chazot Fiona C. Shenton Walter Schunack Daniela Grandi Giuseppina Morini

Alpha (finance)

10.1007/s00011-006-0509-7

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Citations (3)

Characterization of gastrointestinal spasmolytic activity of a new antimuscarinic benzodiazepinone derivative (DF 545)

Pharmacological Research Communications (1988)

M Impicciatore M. Chiavarini Giuseppina Morini Elisabetta Barocelli Giancarlo Tonon

Derivative (finance)

10.1016/s0031-6989(88)80327-8

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Citations (0)

ChemInform Abstract: Heteroarylaminoethyl and Heteroarylthioethylimidazoles. Synthesis and H3‐Receptor Affinity.

ChemInform (1996)

Pier Vincenzo Plazzi Fabrizio Bordi Marco Mor C. Silva Giuseppina Morini

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

10.1002/chin.199610186

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Citations (0)

Comparison of the protective effect of (R)-α-methylhistamine and its prodrugs on gastric mucosal damage induced by ethanol in the rat

General Pharmacology The Vascular System (1996)

Giuseppina Morini Daniela Grandi G. Bertaccini

Mucosal lesions

10.1016/s0306-3623(96)00068-7

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Citations (3)

Are histamine receptors involved in the stimulant activities of thiazolylethylamines supposed as cyclic models of dimaprit?

Agents and Actions (1987)