Netazepide, a gastrin/CCK2 receptor antagonist, causes dose‐dependent, persistent inhibition of the responses to pentagastrin in healthy subjects

摘要: Aims To confirm by means of pentagastrin, a synthetic gastrin agonist, that netazepide is gastrin/CCK2 receptor antagonist in healthy subjects, and antagonism persists during repeated dosing. Methods We did two studies which we infused pentagastrin (0.6 μg kg−1 h−1 intravenously), aspirated gastric secretion measured the volume, pH H+ rate aspirate. First, double-blind, five-way crossover study (n = 10) to assess effect single oral doses (1, 5, 25 100 mg) placebo on response pentagastrin. Then, single-blind, placebo-controlled 8) first last (100 mg) twice daily for 13 pentagastrin. Results Netazepide was well tolerated. After placebo, increased volume reduced Compared with caused dose-dependent inhibition (P < 0.02); abolished response. doses, reduction persisted 0.001), but mostly lost. Conclusions Netazepide an orally active, potent, competitive human receptors. Antagonism dose dependent dosing, despite tolerance pH. Further are required explain tolerance. Netazepide tool physiology pharmacology gastrin, merits patients its potential treat acid-related conditions trophic effects hypergastrinaemia.