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O primeiro frmaco desta classe aprovado para uso teraputico em 2006 pelo FDA foi a sitaglipitina, obtida aps uma srie de otimizaes estruturais a partir de ligantes identificados por triagem robotizada de alto rendimento

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Hence, mice lacking GLP-1R only in the peripheral nervous system (PNS) or central nervous system have normal ip and oral glucose tolerance as compared to controls (Sisley et al., 2014)