Chang R S, Lotti V J, Keegan M E, Kunkel K A
Biochem Biophys Res Commun. 1986 Jan 29;134(2):895-9. doi: 10.1016/s0006-291x(86)80504-6.
The binding of [3H]pentagastrin to guinea pig gastric glands was specific, saturable and of high affinity (Kd = 5 nM). The relative order of potencies for gastrin and CCK analogs in displacing [3H]pentagastrin binding correlated well with those obtained using [125I]gastrin and their reported biological potencies for stimulating acid secretion. Nonselective CCK/gastrin antagonists including carbobenzoxy-CCK (26-32), proglumide and benzotript, but not the selective peripheral CCK antagonist, asperlicin, inhibited specific [3H]pentagastrin binding. The results indicate that [3H]pentagastrin labels physiologically relevant gastrin receptors in guinea pig gastric glands.
[3H]五肽胃泌素与豚鼠胃腺的结合具有特异性、可饱和性且亲和力高（解离常数Kd = 5 nM）。胃泌素和胆囊收缩素类似物在取代[3H]五肽胃泌素结合方面的效价相对顺序，与使用[125I]胃泌素获得的结果及其报道的刺激胃酸分泌的生物学效价密切相关。包括苄氧羰基-胆囊收缩素（26-32）、丙谷胺和苯曲嗪在内的非选择性胆囊收缩素/胃泌素拮抗剂可抑制特异性[3H]五肽胃泌素结合，但选择性外周胆囊收缩素拮抗剂阿哌立定则无此作用。结果表明，[3H]五肽胃泌素标记了豚鼠胃腺中与生理相关的胃泌素受体。
