有机溶剂中青霉素酰化酶催化的动力学与热力学

用电泳纯巨大芽孢杆菌胞外青霉素酸化酶,研究其在乙醇、正丙醇、异丙醇、正丁醇、丙酮、二氧六环、四氢呋喃等有机溶剂存在下的动力学和热力学特性,并与相应的溶液酶作比较,探讨溶剂酶（有机溶剂存在下的酶）和溶液酶在催化活性及分于构象方面的特性。     

THE USE OF PHOSPHOLIPASE C IN THE STUDY OF RECEPTORS FOR NEUROMUSCULAR BLOCKING AGENTS

Abstract— Segments of diaphragmatic muscle and cerebral nerve-ending particles from the rat were treated exhaustively (180 min) with high concentrations of phospholipase C (300 μg/ml) (EC 3.1.4.3). This enzyme caused loss of approx. 50 per cent of muscle membrane P and 70 per cent of nerve-ending membrane P. At lower concentrations (3 μg/ml; 180 min), phospholipase C released 25 per cent muscle membrane P and 55 per cent of nerve-ending membrane P. At the lower concentration (3 μg/ml; 180 min), the enzyme caused a slow but progressive loss (90 per cent) of muscle twitch amplitude evoked by nerve stimulation (phrenic nerve-hemidiaphragm preparation). Loss of muscle twitch amplitude was notably slowed by removal of the enzyme. Phospholipase C-treated neuromuscular junctions developed no resistance to hemicholinium, botulinum toxin, or d-tubocurarine. Such preparations were unusually sensitive to the neuromuscular blocking action of di-isopropylfluorophosphate. The data do not encourage a belief that phospholipids which are substrates for phospholipase C are receptors for hemicholinium, botulinum toxin, d-tubocurarine or di-isopropylfluorophosphate.     

STABILITY OF SYNAPTOSOMAL GABA LEVELS AND THEIR USE IN DETERMINING THE IN VIVO EFFECTS OF DRUGS: CONVULSANT AGENTS

—The stability of the GABA content of synaptosomal-enriched fractions was evaluated by two approaches. Firstly, the addition of 10^?3m -aminooxyacetic acid to the homogenizing medium totally inhibited the GABA-degrading enzyme in the fractions but did not affect the GABA levels. This indicated that GABA was not being metabolized during the normal preparation of the synaptosomal-enriched fraction. Secondly, when synaptosomal-enriched fractions were re-fractionated by discontinuous density gradient centrifugation, the GABA contents of the fractions before and after the second fractionation were very similar provided they were expressed on a per mg protein basis. It was therefore concluded that the GABA content of the organelles was not subject to change during the fractionation procedures. On the basis of these findings and others it was suggested that the synaptosomal-enriched fraction could be used as a model to evaluate drug-induced changes in GABA levels in nerve endings. In vivo experimentation indicated that the convulsant agents hydrazine, isonicotinic acid hydrazide and aminooxyacetic acid brought about similar decreases in the GABA content of the synaptosomal-enriched fractions prepared from tissue at the onset of seizures despite the fact that no correlation was observed between seizure activity and whole brain GABA levels.     

THE USE OF BENZOCAINE HYDROCHLORIDE AS FISH TRANQUILLIZER AND ANAESTHETIC IN SALINE WATERS

SUMMARY

The anaesthetic effects of various concentrations of benzocaine hydrochloride were tested on Liza macrolepis and Sarotherodor mossambicus in sea water and diluted sea water, respectively. Induction time for anaesthesia was negatively correlated with increasing anaesthetic concentrations in L. macrolepis.

In S. mossambicus, however, operculum clamping appeared to be responsible-f or induction times increasing with increased anaesthetic concentration.

The tranquillizing effects of low concentrations of benzocaine hydrochloride on L. macrolepis was also studied.