Edwards S R, Shanley B C, Reynoldson J A
Neuropharmacology. 1984 Apr;23(4):477-81. doi: 10.1016/0028-3908(84)90259-4.
Delta-aminolaevulinic acid (ALA) is suspected of being responsible for the neuropsychiatric symptoms of acute porphyria. The object of this study was to examine the effects of ALA in vivo on a range of behavioural and physiological functions which are known to be affected in the acute porphyric attack. Aminolaevulinic acid was administered by intraperitoneal or subcutaneous injection to mice in doses up to 1000 mg/kg and effects on nociception (hot-plate and abdominal constriction tests), CNS excitability (pentobarbitone sleep-time and pentylenetetrazole-induced seizures), motor co-ordination and grip (rotating rod test) were studied. Rats were given intravenous injections or infusions of ALA of up to 24 mg and changes in blood pressure, heart rate and ED50 for noradrenaline, acetylcholine and isoprenaline examined. No statistically significant effects were noted, using buffered solutions of ALA (pH 7.0-7.4). However, unbuffered solutions of ALA caused significant bradycardia and hypotension. These results do not support the hypothesis that ALA has significant acute neuropharmacological activity in vivo when the blood-brain barrier is intact.
δ-氨基乙酰丙酸（ALA）被怀疑是急性卟啉症神经精神症状的病因。本研究的目的是检测ALA在体内对一系列行为和生理功能的影响，这些功能在急性卟啉症发作时已知会受到影响。以高达1000mg/kg的剂量通过腹腔或皮下注射给小鼠施用氨基乙酰丙酸，并研究其对痛觉（热板和腹部收缩试验）、中枢神经系统兴奋性（戊巴比妥睡眠时间和戊四氮诱发的惊厥）、运动协调性和握力（转棒试验）的影响。给大鼠静脉注射或输注高达24mg的ALA，并检测去甲肾上腺素、乙酰胆碱和异丙肾上腺素的血压、心率和半数有效量（ED50）的变化。使用ALA缓冲溶液（pH 7.0 - 7.4）时未观察到统计学上的显著影响。然而，未缓冲的ALA溶液导致显著的心动过缓和低血压。这些结果不支持在血脑屏障完整时ALA在体内具有显著急性神经药理活性的假说。
