Li F F, Fu S X, Li Y S
Department of Pharmacology, Hebei Medical College, Shijiazhuang, China.
Zhongguo Yao Li Xue Bao. 1992 Jan;13(1):59-62.
m-Nisoldipine (m-Nis) and nisoldipine (Nis) inhibited spontaneous contraction of isolated non-pregnant human myometrium, IC50 being 3.7 +/- 0.7 mumol.L-1 for m-Nis and 6.0 +/- 0.9 mumol.L-1 for Nis. Both drugs also suppressed spontaneous and oxytocin-induced contraction of isolated pregnant rat uterus. In isolated uterus from virgin rat, both drugs inhibited the contractions induced by KCl, acetylcholine (ACh), and oxytocin (Oxy), the values of pD'2 against KCl, ACh, Oxy being 9.0 +/- 0.2, 6.1 +/- 0.1, and 5.9 +/- 0.1 for m-Nis and 9.1 +/- 0.3, 5.7 +/- 0.2, and 5.6 +/- 0.1 for Nis respectively. The results indicate that both m-Nis and Nis may be clinically useful for the treatment of dysmenorrhea and premature labour.
间尼索地平（m-Nis）和尼索地平（Nis）可抑制离体未孕人子宫肌层的自发收缩，m-Nis的半数抑制浓度（IC50）为3.7±0.7μmol·L-1，Nis为6.0±0.9μmol·L-1。两种药物还可抑制离体妊娠大鼠子宫的自发收缩和催产素诱导的收缩。在未交配大鼠的离体子宫中，两种药物均可抑制氯化钾、乙酰胆碱（ACh）和催产素（Oxy）诱导的收缩，m-Nis对氯化钾、ACh、Oxy的亲和力指数（pD'2）值分别为9.0±0.2、6.1±0.1和5.9±0.1，Nis分别为9.1±0.3、5.7±0.2和5.6±0.1。结果表明，m-Nis和Nis在临床上可能对痛经和早产的治疗有效。
