Gardiner J E, Gwee M C
Br J Pharmacol. 1977 Jul;60(3):351-6. doi: 10.1111/j.1476-5381.1977.tb07507.x.
1 The effects of hemicholinium no. 3 (HC-3) and its p-terphenyl analogue (TPHC-3) on the disposition and distribution of free choline were studied in rabbits under pentobarbitone anaesthesia. Free choline was determined by bioassay. 2 The respiration of animals given 0.35 mumol/kg of HC-3 was hardly affected; however, 4 out of 6 rabbits given the same dose of TPHC-3 exhibited varying degrees of respiratory impairment. All animals that received 2 injections (1 h apart) of either HC-3 (1.4 mumol/kg) or TPHC-3 (0.7 mumol/kg) developed respiratory difficulty about 1 h after the second injection. 3 The respiratory distress was accompanied by a 2 to 15-fold rise in plasma choline concentration. This rise has been attributed to hypoxia. 4 In experiments in which choline has been infused it was observed that HC-3 could impair the animal's ability to dispose of exogenous choline. In control rabbits neither HC-3 nor TPHC-3 produced changes in plasma choline concentrations unless the respiration was depressed. 5 Either HC-3 or TPHC-3 (both at 0.35 mumol/kg) significantly (P less than 0.05) reduced the kidney choline concentration by 40% and 30% respectively; both hemicholiniums raised the lung choline concentration by about 35%. Only TPHC-3 caused a significant rise (40%) in liver choline. The choline concentrations in other tissues were unaffected by the hemicholiniums.
在戊巴比妥麻醉下,研究了3号半胆碱(HC - 3)及其对三联苯类似物(TPHC - 3)对家兔游离胆碱处置和分布的影响。游离胆碱通过生物测定法测定。
给予0.35 μmol/kg HC - 3的动物呼吸几乎未受影响;然而,给予相同剂量TPHC - 3的6只家兔中有4只表现出不同程度的呼吸损伤。所有接受两次注射(间隔1小时),剂量分别为HC - 3(1.4 μmol/kg)或TPHC - 3(0.7 μmol/kg)的动物在第二次注射后约1小时出现呼吸困难。
呼吸窘迫伴随着血浆胆碱浓度升高2至15倍。这种升高归因于缺氧。
在胆碱输注实验中观察到,HC - 3会损害动物处置外源性胆碱的能力。在对照家兔中,除非呼吸受到抑制,否则HC - 3和TPHC - 3均不会引起血浆胆碱浓度变化。
HC - 3或TPHC - 3(均为0.35 μmol/kg)分别使肾脏胆碱浓度显著(P小于0.05)降低40%和30%;两种半胆碱均使肺胆碱浓度升高约35%。只有TPHC - 3使肝脏胆碱显著升高(40%)。半胆碱对其他组织中的胆碱浓度无影响。