Coruzzi G, Poli E
Gen Pharmacol. 1987;18(1):69-74. doi: 10.1016/0306-3623(87)90172-8.
The inhibitory action of nifedipine, verapamil, diltiazem and trifluoperazine has been examined on isolated duodenum from rats and rabbits. On rabbit duodenum Ca2+ antagonists caused a reduction of the spontaneous motility in very low concentrations (10(-12)-10(-6)M). On rat duodenum Ca2+ antagonists inhibited the contractile response to BaCl2, CaCl2 and to field stimulation, nifedipine being the most potent compound (threshold concentration down to 10(-12)M). The above results indicated that Ca2+ antagonists can markedly alter the duodenal motility, both basal and drug-stimulated. The high potency of nifedipine and the selective antagonism by Bay K 8644 against nifedipine suggest the presence of a specific receptor for the dihydropyridines (DHP receptor) in the duodenum.
已对硝苯地平、维拉帕米、地尔硫卓和三氟拉嗪对大鼠和家兔离体十二指肠的抑制作用进行了研究。在家兔十二指肠中,钙拮抗剂在极低浓度(10⁻¹² - 10⁻⁶M)时就会引起自发运动性降低。在大鼠十二指肠中,钙拮抗剂抑制对氯化钡、氯化钙和场刺激的收缩反应,硝苯地平是最有效的化合物(阈值浓度低至10⁻¹²M)。上述结果表明,钙拮抗剂可显著改变十二指肠的基础运动和药物刺激后的运动。硝苯地平的高效性以及Bay K 8644对硝苯地平的选择性拮抗作用表明,十二指肠中存在二氢吡啶类(DHP受体)的特异性受体。