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ADME studies and preliminary safety pharmacology of LDT5, a lead compound for the treatment of benign prostatic hyperplasia BJMBR
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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Matrix metalloproteinases 2 and 9 expression in canine normal prostate and with proliferative disorders Ciência Rural
Faleiro,Mariana Batista Rodrigues; Croce,Giuliana Brasil; Toledo,Denise Caroline; Rodrigues,Marcela Marcondes Pinto; Batista,Aline Carvalho; Damasceno,Adilson Donizeti; Brito,Luiz Augusto Batista; Amorim,Renée Laufer; Moura,Veridiana Maria Brianezi Dignani de.
In this study the expression of metalloproteinases 2 (MMP-2) and 9 (MMP-9) in canine normal prostates and with proliferative disorders was evaluated to verify the role of these enzymes in extracellular matrix remodeling (ECM) and in the tissue invasion process. A total of 355 prostatic samples were obtained, from which 36 (10.1%) were normal prostates, 46 (13.0%) with benign prostatic hyperplasia (BPH), 128 (36.1%) with proliferative inflammatory atrophy (PIA), 74 (20.8%) with prostatic intraepithelial neoplasia (PIN), and 71 (20.0%) with prostatic carcinoma (PC). Difference in cytoplasmic immunohistochemical staining of MMP-2 and MMP-9 between acinar epithelium and periacinar stroma was found regarding the different diagnosis. The correlation between...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Dog; Gelatinases; Benign prostatic hyperplasia; Proliferative inflammatory atrophy; Prostatic intraepithelial neoplasia; Prostatic carcinoma.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782013000600015
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Prostatic and testicular hemodynamic changes in dogs with untreated benign prostatic hyperplasia and treated with finasteride MV&Z
Angrimani, Daniel de Souza Ramos; Brito, Maíra Morales; Abreu, Renata Azevedo de; Almeida, Leticia Lima de; Nichi, Marcílio; Vannucchi, Camila Infantosi.
The aim of this study was to evaluate the effects of finasteride treatment on prostatic and testicular hemodynamic and vascular variables in dogs with benign prostatic hyperplasia (BPH). Ten dogs aged between 5 and 13 years were selected and assigned to two experimental groups: dogs with BPH (BPH, n=5), and dogs with BPH treated with finasteride (BPH+F, n=5). Three monthly evaluations were performed (day 0 – onset of finasteride treatment, day 30 and day 60). Testicular and prostatic volumes were measured through mode-B ultrasound; prostatic vascularization score (1-3) was measured with the color Doppler ultrasound; and the hemodynamic profile of the prostatic and testicular arteries was measured with spectral Doppler. A reduction of 35.2% in the prostate...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Benign prostatic hyperplasia; Doppler ultrasonography; Dogs hiperplasia prostática benigna; Ultrassonografia doppler; Cães.
Ano: 2017 URL: http://www.revistamvez-crmvsp.com.br/index.php/recmvz/article/view/36767
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