化合物D - 600（甲氧基维拉帕米）对大鼠肾小管糖异生及α - 肾上腺素能刺激加速该过程的影响。 - Suppr

Tubule fragments were isolated from renal cortex of fed rats and glucose formation was measured after incubation with 5 mM-sodium lactate. 20 Compound D-600 (10-100 microM) decreased gluconeogenesis from lactate. This inhibition of the process by compound D-600 increased with increasing extracellular Ca2+ concentration, was overridden by noradrenaline and diminished by starvation for 24 h. 3. Inhibition of lactate-supported gluconeogenesis by compound D-600 was not prevented by the alpha 1-adrenoceptor antagonist thymoxamine. 4. Compound D-600 had little effect on gluconeogenesis from 2-oxoglutarate and increased gluconeogenesis from succinate. 5. Compound D-600 opposed stimulation of gluconeogenesis by noradrenaline or oxymetazoline (a selective alpha-adrenoceptor agonist) in a manner suggesting that compound D-600 is an alpha-adrenoceptor blocker. Oxymetazoline was more sensitive than noradrenaline to blockade by both compound D-600 and by the conventional alpha-adrenoceptor antagonist phentolamine. Noradrenaline became more sensitive to blockade by compound D-600 when extracellular Ca2+ was decreased. 6. Compound D-600 did not block stimulation of gluconeogenesis by angiotensin or cyclic AMP.

从喂食大鼠的肾皮质中分离出肾小管片段，在与5 mM乳酸钠孵育后测量葡萄糖生成量。20化合物D - 600（10 - 100 microM）可降低由乳酸生成葡萄糖的过程。化合物D - 600对该过程的抑制作用随细胞外Ca2 +浓度升高而增强，去甲肾上腺素可消除这种抑制作用，饥饿24小时可使其减弱。
化合物D - 600对乳酸支持的糖异生作用的抑制不能被α1 - 肾上腺素能受体拮抗剂噻吗洛尔阻止。
化合物D - 600对由2 - 氧代戊二酸生成葡萄糖的过程影响很小，却增加了由琥珀酸生成葡萄糖的过程。
化合物D - 600以一种表明其为α - 肾上腺素能受体阻滞剂的方式对抗去甲肾上腺素或奥昔麻黄碱（一种选择性α - 肾上腺素能受体激动剂）对糖异生的刺激作用。奥昔麻黄碱比去甲肾上腺素对化合物D - 600和传统α - 肾上腺素能受体拮抗剂酚妥拉明的阻断作用更敏感。当细胞外Ca2 +减少时，去甲肾上腺素对化合物D - 600的阻断作用变得更敏感。
化合物D - 600不阻断血管紧张素或环磷酸腺苷对糖异生的刺激作用。

化合物D - 600（甲氧基维拉帕米）对大鼠肾小管糖异生及α - 肾上腺素能刺激加速该过程的影响。