哌仑西平和阿托品对卡巴胆碱诱导的离体胃腺胃蛋白酶原分泌影响的差异。

Difference in effects of pirenzepine and atropine on carbachol-induced pepsinogen secretion from isolated gastric glands.

作者信息

Sakamoto C, Matozaki T, Nagao M, Baba S

出版信息

Biochem Biophys Res Commun. 1986 Apr 14;136(1):193-9. doi: 10.1016/0006-291x(86)90894-6.

Abstract

The effect of pirenzepine on carbamylcholine (carbachol)-stimulated pepsinogen secretion was compared with that of atropine in the isolated guinea pig gastric glands. Pirenzepine and atropine caused a dose dependent inhibition of carbachol-stimulated pepsinogen secretion. Moreover, pirenzepine as well as atropine produced a rightward shift in the dose response curve of carbachol-stimulated pepsinogen secretion but did not alter the maximum increase in pepsinogen secretion. Results therefore demonstrate that pirenzepine acts as a specific receptor antagonist in the interaction of carbachol with its receptor on gastric chief cells. However, pirenzepine was 50 times less potent than atropine in inhibiting pepsinogen secretion. Half maximal inhibitory concentration of pirenzepine was 2 X 10(-5) M when a maximally effective concentration of carbachol was used, while that of atropine was 4 X 10(-7) M. Results, therefore, suggest that muscarinic receptor on gastric chief cells to which pirenzepine binds may be an intermediate affinity type.

摘要

在分离的豚鼠胃腺中，比较了哌仑西平与阿托品对氨甲酰胆碱（卡巴胆碱）刺激的胃蛋白酶原分泌的影响。哌仑西平和阿托品对卡巴胆碱刺激的胃蛋白酶原分泌均产生剂量依赖性抑制。此外，哌仑西平和阿托品均使卡巴胆碱刺激的胃蛋白酶原分泌的剂量反应曲线向右移动，但未改变胃蛋白酶原分泌的最大增加量。因此，结果表明哌仑西平在卡巴胆碱与其在胃主细胞上的受体相互作用中起特异性受体拮抗剂的作用。然而，哌仑西平在抑制胃蛋白酶原分泌方面的效力比阿托品低50倍。当使用最大有效浓度的卡巴胆碱时，哌仑西平的半数最大抑制浓度为2×10⁻⁵M，而阿托品的半数最大抑制浓度为4×10⁻⁷M。因此，结果表明哌仑西平所结合的胃主细胞上的毒蕈碱受体可能是中等亲和力类型。