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Discovery of a novel series of orally bioavailable and CNS penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) non-competitive antagonists based on a 1,3-disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione core
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(In fact, exendin-4 has to be cleared out through the kidneys, which takes time.) Successful clinical trials in humans were conducted in the early 2000s
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Risk factors Dose and treatment duration The higher the dose and the longer the treatment duration, the higher the incidence of adverse reactions
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