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Dopaminergic profile of new heterocyclic N-phenylpiperazine derivatives BJMBR
Neves,G.; Fenner,R.; Heckler,A.P.; Viana,A.F.; Tasso,L.; Menegatti,R.; Fraga,C.A.M.; Barreiro,E.J.; Dalla-Costa,T.; Rates,S.M.K..
Dopamine constitutes about 80% of the content of central catecholamines and has a crucial role in the etiology of several neuropsychiatric disorders, including Parkinson's disease, depression and schizophrenia. Several dopaminergic drugs are used to treat these pathologies, but many problems are attributed to these therapies. Within this context, the search for new more efficient dopaminergic agents with less adverse effects represents a vast research field. The aim of the present study was to report the structural design of two N-phenylpiperazine derivatives, compound 4: 1-[1-(4-chlorophenyl)-1H-4-pyrazolylmethyl]-4-phenylhexahydropyrazine and compound 5: 1-[1-(4-chlorophenyl)-1H-1,2,3-triazol-4-ylmethyl]-4-phenylhexahydropyrazine, planned to be dopamine...
Tipo: Info:eu-repo/semantics/other Palavras-chave: N-phenylpiperazine derivatives; Dopamine; Apomorphine hypothermia; Amphetamine stereotypy; Catalepsy.
Ano: 2003 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2003000500010
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Protective effects of phosphodiesterase inhibitors on lung function and remodeling in a murine model of chronic asthma BJMBR
Campos,H.S.; Xisto,D.G.; Oliveira,M.B.G.; Teixeira,I.; Negri,E.M.; Mauad,T.; Carnielli,D.; Lima,L.M.; Barreiro,E.J.; Faffe,D.S.; Zin,W.A.; Lapa e Silva,J.R.; Rocco,P.R.M..
The aim of the present study was to compare the efficacy of a novel phosphodiesterase 4 and 5 inhibitor, LASSBio596, with that of dexamethasone in a murine model of chronic asthma. Lung mechanics (airway resistance, viscoelastic pressure, and static elastance), histology, and airway and lung parenchyma remodeling (quantitative analysis of collagen and elastic fiber) were analyzed. Thirty-three BALB/c mice were randomly assigned to four groups. In the asthma group (N = 9), mice were immunized with 10 µg ovalbumin (OVA, ip) on 7 alternate days, and after day 40 they were challenged with three intratracheal instillations of 20 µg OVA at 3-day intervals. Control mice (N = 8) received saline under the same protocol. In the dexamethasone (N = 8) and LASSBio596...
Tipo: Info:eu-repo/semantics/other Palavras-chave: Asthma; Lung function; Steroid; Phosphodiesterase inhibitors; BALB/c mice.
Ano: 2006 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2006000200016
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Impairment of locomotor activity induced by the novelN-acylhydrazone derivatives LASSBio-785 and LASSBio-786 in mice BJMBR
Silva,G.A.P.; Kummerle,A.E.; Antunes,F.; Fraga,C.A.M.; Barreiro,E.J.; Zapata-Sudo,G.; Sudo,R.T..
The N-acylhydrazone (NAH) analogues N-methyl 2-thienylidene 3,4-benzoylhydrazine (LASSBio-785) and N-benzyl 2-thienylidene 3,4-benzoylhydrazine (LASSBio-786) were prepared from 2-thienylidene 3,4-methylenedioxybenzoylhydrazine (LASSBio-294). The ability of LASSBio-785 and LASSBio-786 to decrease central nervous system activity was investigated in male Swiss mice. LASSBio-785 or LASSBio-786 (30 mg/kg, ip) reduced locomotor activity from 209 ± 26 (control) to 140 ± 18 (P < 0.05) or 146 ± 15 crossings/min (P < 0.05), respectively. LASSBio-785 (15 or 30 mg/kg, iv) also reduced locomotor activity from 200 ± 15 to 116 ± 29 (P < 0.05) or 60 ± 16 crossings/min (P < 0.01), respectively. Likewise, LASSBio-786 (15 or 30 mg/kg, iv) reduced locomotor...
Tipo: Info:eu-repo/semantics/article Palavras-chave: N-acylhydrazone; Locomotor activity; Sedation; Hypnosis; Benzodiazepine receptor; Flumazenil.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013000300263
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