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PubMed1992

In search of a correlation between the electron affinity and the radiosensitizing activity of some glyoxylic compounds.

The electron affinity of some glyoxylic compounds with radiosensitizing properties was evaluated using different approaches. The half-wave reduction potentials were measured by polarography, and the molecular structures in solution were determined by NMR spectroscopy. The electron affinity of the unhydrated and hydrated molecules was theoretically evaluated by means of a semi-empirical quantum mechanical procedure, the MNDO. The possible correlations between these values and the radiosensitizing efficiency of these glyoxylic compounds is discussed.

Electrochemistry↗
PubMed1992

Inhibitory effect of inaperisone hydrochloride (inaperisone), a new centrally acting muscle relaxant, on the micturition reflex.

We examined the effects of inaperisone hydrochloride (inaperisone), a new centrally acting muscle relaxant, on bladder function in anesthetized rats and isolated rat tissues. We also investigated its mechanism of action. When a balloon inserted into the bladder was expanded, rhythmic bladder contractions were observed; inaperisone (4 mg/kg i.v.) abolished these contractions, in both normal and decerebrated rats. The bladder tonus or bladder contraction induced by peripheral stimulation of the pelvic nerve was barely inhibited by inaperisone (4 mg/kg i.v.), but this dose of inaperisone abolished the efferent discharge from the pelvic nerve that accompanied the rhythmic bladder contractions. The doses of intracerebroventricularly (i.c.v.) and intrathecally injected inaperisone which abolished the rhythmic bladder contractions were 10 and 100 micrograms, respectively. The inhibitory effects of inaperisone (4 mg/kg i.v.) were not diminished by naloxone (1 mg/kg i.v.) or by bicuculline (0.5 mg/kg i.v.), but were diminished by phaclofen (30 mg/kg i.v. or 300 micrograms i.c.v.). The specific binding of [3H]baclofen to rat brain synaptosomal membranes was barely inhibited by inaperisone (up to 1 mM). From these results, it is speculated that, among other possible mechanisms, inaperisone inhibits the micturition reflex by acting indirectly on GABAB receptors in the brainstem.

Anesthesia↗
PubMedDate not supplied

Dietary cyclandelate decreases pre-established atherosclerosis in the rabbit.

Rabbits were given a diet containing 1% (w/w) cholesterol for 7 weeks to initiate atherosclerosis and then transferred to a low-cholesterol diet (regression diet) with or without 0.5% (w/w) cyclandelate for 10 weeks. In those fed regression diet alone aortic atherosclerosis increased significantly. Cyclandelate treatment decreased the extent and severity of aortic atherosclerosis. Thus in rabbits receiving cyclandelate the total cholesterol and calcium content of aorta was decreased by 45% and 69% of control values, respectively. The effects of cyclandelate occurred without significant lowering of serum cholesterol or alteration of cholesterol content of liver or calcium content of serum, liver or muscle. The result suggests a specific action of cyclandelate on atheromatous accumulations of the aortic wall.

Animals↗