人降钙素基因相关肽对豚鼠壁细胞制剂胃酸分泌具有皮摩尔效力的抑制作用。

Inhibition of gastric acid secretion by human calcitonin gene-related peptide with picomolar potency in guinea-pig parietal cell preparations.

作者信息

Umeda Y, Okada T

出版信息

Biochem Biophys Res Commun. 1987 Jul 31;146(2):430-6. doi: 10.1016/0006-291x(87)90547-x.

Abstract

The effect of CGRP on [14C]-aminopyrine accumulation in isolated parietal cell preparations from guinea-pig fundic mucosa was studied. Parietal cells consisted of 60% of the preparations. [14C]-Aminopyrine accumulation was used as an index of physiological response of parietal cells to secretagogues. CGRP dose-dependently (10(-12)-10(-9) M) inhibited parietal cell aminopyrine accumulation stimulated by histamine (10(-4) M), carbachol (10(-4) M), and pentagastrin (5 X 10(-6) M). The concentration of CGRP exerting half-maximal inhibition of [14C]-aminopyrine accumulation was 8.7 X 10(-11) M for histamine, 9.1 X 10(-11) M for carbachol, and 4.7 X 10(-11) M for pentagastrin. The inhibitory effect was much more potent than cimetidine, pirenzepine or benzotript. CGRP but not cimetidine inhibited DBcAMP stimulated aminopyrine accumulation (IC50 = 7.5 X 10(-11) M). These results suggest that CGRP may exert its inhibitory action on gastric acid secretion by a direct action on the parietal cell or the somatostatin-producing D cell.

摘要

研究了降钙素基因相关肽（CGRP）对豚鼠胃底黏膜分离壁细胞制剂中[¹⁴C] - 氨基比林蓄积的影响。壁细胞占制剂的60%。[¹⁴C] - 氨基比林蓄积用作壁细胞对促分泌剂生理反应的指标。CGRP以剂量依赖性方式（10⁻¹² - 10⁻⁹ M）抑制组胺（10⁻⁴ M）、卡巴胆碱（10⁻⁴ M）和五肽胃泌素（5×10⁻⁶ M）刺激的壁细胞氨基比林蓄积。对[¹⁴C] - 氨基比林蓄积产生半数最大抑制作用时，CGRP的浓度对组胺为8.7×10⁻¹¹ M，对卡巴胆碱为9.1×10⁻¹¹ M，对五肽胃泌素为4.7×10⁻¹¹ M。其抑制作用比西咪替丁、哌仑西平或苯佐曲普更有效。CGRP而非西咪替丁抑制二丁酰环磷腺苷（DBcAMP）刺激的氨基比林蓄积（IC₅₀ = 7.5×10⁻¹¹ M）。这些结果表明，CGRP可能通过直接作用于壁细胞或产生生长抑素的D细胞对胃酸分泌发挥抑制作用。