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@ARTICLE{Godin:284096,
author = {Godin, Adriana M. and Araújo, Débora P. and Menezes,
Raquel R. and Brito, Ana Mercy S. and Melo, Ivo S. F. and
Coura, Giovanna M. E. and Soares, Darly G. and Bastos,
Leandro F. S. and Amaral, Flávio A. and Secchim Ribeiro,
Lucas and Boff, Daiane and Santos, Julliana R. A. and
Santos, Daniel A. and Teixeira, Mauro M. and de Fátima,
Ângelo and Machado, Renes R. and Coelho, Márcio M.},
title = {{A}ctivities of 2-phthalimidethanol and 2-phthalimidethyl
nitrate, phthalimide analogs devoid of the glutarimide
moiety, in experimental models of inflammatory pain and
edema},
journal = {Pharmacology, biochemistry and behavior},
volume = {122},
issn = {0091-3057},
address = {Amsterdam [u.a.]},
publisher = {Elsevier Science},
reportid = {DZNE-2026-00104},
pages = {291 - 298},
year = {2014},
abstract = {The reintroduction of thalidomide in the pharmacotherapy
greatly stimulated the interest in the synthesis and
pharmacological evaluation of phthalimide analogs with new
and improved activities and also greater safety. In the
present study, we evaluated the activities of two
phthalimide analogs devoid of the glutarimide ring, namely
2-phthalimidethanol (PTD-OH) and 2-phthalimidethyl nitrate
(PTD-NO), in experimental models of inflammatory pain and
edema in male C57BL/6J mice. Intraplantar (i.pl.) injection
of carrageenan (300 μg) induced mechanical allodynia and
this response was inhibited by previous per os (p.o.)
administration of PTD-OH and PTD-NO (750 mg/kg) and also by
thalidomide (500 or 750 mg/kg). The edema induced by
carrageenan was also inhibited by previous p.o.
administration of PTD-OH (500 and 750 mg/kg) and PTD-NO
(125, 250, 500 or 750 mg/kg), but not by thalidomide.
Carrageenan increased tumor necrosis factor (TNF)-α and
CXCL1 concentrations and also the number of neutrophils in
the paw tissue. Previous p.o. administration of PTD-NO (500
mg/kg) reduced all the parameters, while PTD-OH (500 mg/kg)
reduced only the accumulation of neutrophils. Thalidomide,
on the other hand, was devoid of effect on these biochemical
parameters. Plasma concentrations of nitrite were increased
after p.o. administration of the phthalimide analog coupled
to a NO donor, PTD-NO (500 mg/kg), but not after
administration of PTD-OH or thalidomide. In conclusion, our
results show that small molecules, structurally much simpler
than thalidomide or many of its analogs under investigation,
exhibit similar activities in experimental models of pain
and inflammation. Finally, as there is evidence that the
glutarimide moiety contributes to the teratogenic effect of
many thalidomide analogs, our results indicate that
phthalimide analogs devoid of this functional group could
represent a new class of analgesic and anti-inflammatory
candidates with potential greater safety.},
keywords = {Animals / Carrageenan: toxicity / Disease Models, Animal /
Edema: chemically induced / Edema: drug therapy / Edema:
metabolism / Inflammation: drug therapy / Inflammation:
metabolism / Ketoglutaric Acids: chemistry / Male / Mice /
Mice, Inbred C57BL / Pain: drug therapy / Pain: metabolism /
Pain Measurement: drug effects / Pain Measurement: methods /
Phthalimides: chemistry / Phthalimides: therapeutic use /
2-Phthalimidethanol (Other) / 2-Phthalimidethyl nitrate
(Other) / Inflammation (Other) / Pain (Other) / Phthalimide
analogs (Other) / Thalidomide (Other) / Ketoglutaric Acids
(NLM Chemicals) / Phthalimides (NLM Chemicals) / phthalimide
(NLM Chemicals) / glutaramic acid (NLM Chemicals) /
Carrageenan (NLM Chemicals)},
ddc = {540},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
doi = {10.1016/j.pbb.2014.04.008},
url = {https://pub.dzne.de/record/284096},
}