Cheuk J M, Hollingsworth M, Hughes S J, Piper I T, Maresh M J
Department of Physiological Sciences, University of Manchester, England.
Am J Obstet Gynecol. 1993 Mar;168(3 Pt 1):953-60. doi: 10.1016/s0002-9378(12)90852-2.
The aim was to investigate the properties of two potassium channel openers in human myometrium.
The abilities of aprikalim and BRL 38227 to inhibit contractions produced by potassium chloride and oxytocin of myometrial strips from nonpregnant and pregnant women were studied.
Aprikalim (1 and 10 mumol/L) and BRL 38227 (1 and 10 mumol/L) suppressed contractions induced by low (10 and 20 mmol/L) but not high (40 and 80 mmol/L) potassium chloride concentrations. Aprikalim and BRL 38227 were also potent relaxants of oxytocin (1 nmol/L)-induced contractions with rapid onset of action, of similar potency to each other, and reversible. Both compounds were significantly more potent against oxytocin (1 nmol/L)-induced contractions in myometrial strips from nonpregnant than from pregnant women. Aprikalim and BRL 38227, as relaxants of oxytocin-induced contractions, were antagonized by glibenclamide (1 mumol/L), a blocker of adenosine 5'-triphosphate-sensitive potassium channels.
The results suggest that aprikalim and BRL 38227 relax the human myometrium by potassium channel opening, possibly at adenosine 5'-triphosphate-sensitive potassium channels. Compounds of this pharmacologic class are useful for investigating the physiologic functions of potassium channels in this tissue and could have a place in the treatment of dysmenorrhea and preterm labor.
旨在研究两种钾通道开放剂在人子宫肌层中的特性。
研究了阿普卡林和BRL 38227抑制非妊娠和妊娠妇女子宫肌条由氯化钾和催产素引起的收缩的能力。
阿普卡林（1和10μmol/L）以及BRL 38227（1和10μmol/L）可抑制低浓度（10和20mmol/L）但不能抑制高浓度（40和80mmol/L）氯化钾诱导的收缩。阿普卡林和BRL 38227也是催产素（1nmol/L）诱导收缩的强效松弛剂，起效迅速，效力相似且作用可逆。这两种化合物对非妊娠妇女子宫肌条中催产素（1nmol/L）诱导的收缩的抑制作用明显强于妊娠妇女。作为催产素诱导收缩的松弛剂，阿普卡林和BRL 38227被格列本脲（1μmol/L）拮抗，格列本脲是一种三磷酸腺苷敏感性钾通道阻滞剂。
结果表明，阿普卡林和BRL 38227可能通过开放三磷酸腺苷敏感性钾通道使人类子宫肌层松弛。这类药理化合物有助于研究该组织中钾通道的生理功能，并且在痛经和早产的治疗中可能占有一席之地。
