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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Cantabrana B, Baamonde A, Andres-Trelles F, Hidalgo A

Departamento de Medicina, Facultad de Medicina, Universidad de Oviedo, Spain.

Gen Pharmacol. 1990;21(1):89-95. doi: 10.1016/0306-3623(90)90601-h.

The effects of 4 inhibitors of eicosanoid synthesis (ESIs)--mepacrine (MEP, 10(-5) - 3 x 10(-4) M), nordihydroguaiaretic acid (NDHGA, 10(-6) - 2 x 10(-5) M), indomethacin (IND, 2 x 10(-6) M and 2 x 10(-5) M) and imidazole (IMI, 10(-5) M and 10(-4) M)--on the motility induced by oxytocin (OT, 0.5 and 4 mU/ml) in uterus of rats in natural oestrus and of ovariectomized rats have been studied. 2. MEP, NDHGA and IND, but not IMI, inhibited the motility induced by both concentrations of OT in natural oestrus. Ovariectomy enhanced the effects of all ESIs, except the one of MEP. 3. MEP and NDHGA, but not IND or IMI, inhibited the contractions induced by methacholine (10(-5) M) and prostaglandin F2a (10(-6) M) and relaxed in a dose-dependent way the tonic component of the contractile response to KCl 60 mM (DI50: 6.14 +/- 0.38 and 1.38 +/- 0.29 x 10(-5) M, respectively). 4. CaCl2 (0.1-10 mM) reverted the relaxation of KCl contractions produced by MEP but not by NDHGA.

研究了4种类花生酸合成抑制剂（ESIs）——米帕林（MEP，10⁻⁵ - 3×10⁻⁴ M）、去甲二氢愈创木酸（NDHGA，10⁻⁶ - 2×10⁻⁵ M）、吲哚美辛（IND，2×10⁻⁶ M和2×10⁻⁵ M）以及咪唑（IMI，10⁻⁵ M和10⁻⁴ M）对处于自然发情期的大鼠子宫和去卵巢大鼠子宫中由催产素（OT，0.5和4 mU/ml）诱导的运动的影响。2. MEP、NDHGA和IND能抑制自然发情期两种浓度OT诱导的运动，而IMI不能。去卵巢增强了所有ESIs的作用，但MEP除外。3. MEP和NDHGA能抑制由乙酰甲胆碱（10⁻⁵ M）和前列腺素F2α（10⁻⁶ M）诱导的收缩，并以剂量依赖方式使对60 mM KCl的收缩反应的强直成分松弛（DI50分别为：6.14±0.38和1.38±0.29×10⁻⁵ M）。4. CaCl₂（0.1 - 10 mM）能逆转MEP导致的KCl收缩的松弛，但不能逆转NDHGA导致的。

Cantabrana B, Baamonde A, Andres-Trelles F, Hidalgo A

Departamento de Medicina, Facultad de Medicina, Universidad de Oviedo, Spain.

Gen Pharmacol. 1990;21(1):89-95. doi: 10.1016/0306-3623(90)90601-h.

The effects of 4 inhibitors of eicosanoid synthesis (ESIs)--mepacrine (MEP, 10(-5) - 3 x 10(-4) M), nordihydroguaiaretic acid (NDHGA, 10(-6) - 2 x 10(-5) M), indomethacin (IND, 2 x 10(-6) M and 2 x 10(-5) M) and imidazole (IMI, 10(-5) M and 10(-4) M)--on the motility induced by oxytocin (OT, 0.5 and 4 mU/ml) in uterus of rats in natural oestrus and of ovariectomized rats have been studied. 2. MEP, NDHGA and IND, but not IMI, inhibited the motility induced by both concentrations of OT in natural oestrus. Ovariectomy enhanced the effects of all ESIs, except the one of MEP. 3. MEP and NDHGA, but not IND or IMI, inhibited the contractions induced by methacholine (10(-5) M) and prostaglandin F2a (10(-6) M) and relaxed in a dose-dependent way the tonic component of the contractile response to KCl 60 mM (DI50: 6.14 +/- 0.38 and 1.38 +/- 0.29 x 10(-5) M, respectively). 4. CaCl2 (0.1-10 mM) reverted the relaxation of KCl contractions produced by MEP but not by NDHGA.

研究了4种类花生酸合成抑制剂（ESIs）——米帕林（MEP，10⁻⁵ - 3×10⁻⁴ M）、去甲二氢愈创木酸（NDHGA，10⁻⁶ - 2×10⁻⁵ M）、吲哚美辛（IND，2×10⁻⁶ M和2×10⁻⁵ M）以及咪唑（IMI，10⁻⁵ M和10⁻⁴ M）对处于自然发情期的大鼠子宫和去卵巢大鼠子宫中由催产素（OT，0.5和4 mU/ml）诱导的运动的影响。2. MEP、NDHGA和IND能抑制自然发情期两种浓度OT诱导的运动，而IMI不能。去卵巢增强了所有ESIs的作用，但MEP除外。3. MEP和NDHGA能抑制由乙酰甲胆碱（10⁻⁵ M）和前列腺素F2α（10⁻⁶ M）诱导的收缩，并以剂量依赖方式使对60 mM KCl的收缩反应的强直成分松弛（DI50分别为：6.14±0.38和1.38±0.29×10⁻⁵ M）。4. CaCl₂（0.1 - 10 mM）能逆转MEP导致的KCl收缩的松弛，但不能逆转NDHGA导致的。