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| Noël,F.; Nascimento-Viana,J.B.; Romeiro,L.A.S.; Silva,R.O.; Lemes,L.F.N.; Oliveira,A.S.; Giorno,T.B.S.; Fernandes,P.D.; Silva,C.L.M.. |
| This study aimed to estimate the absorption, distribution, metabolism and excretion (ADME) properties and safety of LDT5, a lead compound for oral treatment of benign prostatic hyperplasia that has previously been characterized as a multi-target antagonist of α1A-, α1D-adrenoceptors and 5-HT1A receptors. The preclinical characterization of this compound comprised the evaluation of its in vitro properties, including plasma, microsomal and hepatocytes stability, cytochrome P450 metabolism and inhibition, plasma protein binding, and permeability using MDCK-MDR1 cells. De-risking and preliminary safety pharmacology assays were performed through screening of 44 off-target receptors and in vivo tests in mice (rota-rod and single dose toxicity). LDT5 is stable in... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Benign prostatic hyperplasia; ADME; Safety; Permeability; CYP; Preclinical development. |
| Ano: 2016 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2016001200603 |
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| Nicolau,L.A.D.; Silva,R.O.; Damasceno,S.R.B.; Carvalho,N.S.; Costa,N.R.D.; Aragão,K.S.; Barbosa,A.L.R.; Soares,P.M.G.; Souza,M.H.L.P.; Medeiros,J.V.R.. |
| Our objective was to investigate the protective effect of Lawesson's reagent, an H2S donor, against alendronate (ALD)-induced gastric damage in rats. Rats were pretreated with saline or Lawesson's reagent (3, 9, or 27 µmol/kg, po) once daily for 4 days. After 30 min, gastric damage was induced by ALD (30 mg/kg) administration by gavage. On the last day of treatment, the animals were killed 4 h after ALD administration. Gastric lesions were measured using a computer planimetry program, and gastric corpus pieces were assayed for malondialdehyde (MDA), glutathione (GSH), proinflammatory cytokines [tumor necrosis factor (TNF)-α and interleukin (IL)-1β], and myeloperoxidase (MPO). Other groups were pretreated with glibenclamide (5 mg/kg, ip) or with... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Alendronate; Lawesson's reagent; H2S donors; Gastric damage. |
| Ano: 2013 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013000800708 |
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