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Obesity (Silver Spring) ; 19(1): 121-7, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-20559304

RESUMO

Significant weight loss following Roux-en-Y gastric bypass surgery (RYGB) in obese humans correlates with enhanced secretion of anorexigenic gut hormones glucagon-like peptide-1 (GLP-1) and peptide YY(3-36) (PYY(3-36)). Our aim here was to identify a dosing strategy for intraperitoneal (IP) infusion of GLP-1 homologue exendin-4 alone and with PYY(3-36) that produces a sustained reduction in daily food intake and body weight in diet-induced obese (DIO) rats. We tested 12 exendin-4 strategies over 10 weeks. Exendin-4 infused during the first and last 3 h of the dark period at 15-20 pmol/h (0.15 nmol/kg/day) produced a sustained 24 ± 1% reduction in daily food intake for 17 days, and decreased body weight by 7%. In a separate group of DIO rats, none of seven dosing strategies combining exendin-4 and PYY(3-36) produced a similar reduction in daily food intake for >10 days. The subsequent decline in efficacies of exendin-4 alone and with PYY(3-36) on food intake and body weight in each experiment suggested possible receptor downregulation and tolerance to treatments. However, when treatments were discontinued for 1 day following losses in efficacies, daily food intake significantly increased. Together, these results demonstrate that (i) intermittent IP infusion of a low dose of exendin-4 can produce a relatively prolonged reduction in daily food intake and body weight in DIO rats, (ii) co-infusion of exendin-4 and PYY(3-36) does not further prolong this response, and (iii) activation of an orexigenic mechanism gradually occurs to counteract the inhibitory effects of exendin-4 alone and with PYY(3-36) on food intake and body weight.


Assuntos
Peso Corporal/efeitos dos fármacos , Ingestão de Alimentos/efeitos dos fármacos , Obesidade/fisiopatologia , Peptídeo YY/administração & dosagem , Peptídeos/administração & dosagem , Peptídeos/farmacologia , Peçonhas/administração & dosagem , Peçonhas/farmacologia , Animais , Peso Corporal/fisiologia , Dieta/efeitos adversos , Relação Dose-Resposta a Droga , Combinação de Medicamentos , Avaliação Pré-Clínica de Medicamentos , Ingestão de Alimentos/fisiologia , Exenatida , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/farmacologia , Masculino , Obesidade/tratamento farmacológico , Obesidade/etiologia , Fragmentos de Peptídeos , Peptídeo YY/farmacologia , Ratos , Ratos Sprague-Dawley , Redução de Peso/efeitos dos fármacos
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