Benzotript

Benzotript is an gastrin-receptor antagonist, with anti-gastrinic.proglumide and benzotript, a new tryptophan derivative, to inhibit acid output from isolated gastric fundic parietal cells from rabbit. As measured with the [14C]aminopyrine (AP) accumulation method as an index of acid secretion, the two drugs inhibited basal AP with IC-50 values of 1 X 10 (-2) M for proglumide and 1 X 10 (-3) M for benzotript. In the case of secretagogue stimulation (1) benzotript slightly affected histamine-induced AP (15% inhibition at 5 X 10 (-3) M), proglumide did not; (2) both proglumide and benzotript inhibited in a non-competitive manner acetylcholine-induced AP; (3) these isolated cells were sensitive to gastrin and the dose-response curve for the stimulant was biphasic (maximum for 1 X 10 (-9) M), suggesting a desensitization mechanism. Proglumide and benzotript competitively inhibited both [125I]gastrin binding to its receptor sites and gastrin-induced AP, suggesting they are members of a class of gastrin-receptor antagonists.

39544-74-6

>98% (HPLC)

O=C (O) [C@H] (CC1=CNC2=C1C=CC=C2) NC (C3=CC=C (Cl) C=C3) =O

C18H15ClN2O3

342.78

Storage temperature: -20°C. Stability: ≥ 2 years