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Biomedical subjects

J P Fry

Publications and source records attributed to J P Fry.

32 records · Page 2Linked to original sources

Some pharmacological studies on the spastic mouse.

1 Full-wave rectification and integration of the EMG signal recorded from the hamstring muscles of the spastic mouse was used to evaluate the actions of a variety of drugs on the muscle rigidity of these mutants, animals in which no histological lesion has yet been found. 2 Profound and long-lasting muscle relaxant responses were consistently observed upon the injection of diazepam (2 mg/kg, i.p.) and flunitrazepam (2 mg/kg, i.p.). Such responses were always greater than those obtained upon injection of 40% (v/v) propylene glycol (10 ml/kg) alone, the vehicle for the benzodiazepines. 3 The muscle relaxant action of a low dose (0.25 mg/kg i.p.) of the benzodiazepine Roll-6896 was not shared by the same dose of its enantiomer Roll-6893. 4 Profound and long-lasting muscle relaxation was caused by sodium valproate (696 mg/kg, i.p.). Consistent muscle relaxant responses were also observed upon the injection of pentobarbitone (30 mg/kg, i.p.), but not phenobarbitone (30 mg/kg, i.p.). 5 Other drugs that had little or no detectable effect on the muscle rigidity of the spastic mouse included diphenylhydantoin (30 mg/kg, i.p.) and bromocriptine (10 mg/kg, s.c.) while, in some animals, benztropine (2 mg/kg, i.p.) and baclofen (10 mg/kg, i.p.) increased muscle rigidity. 6 The development of full muscle relaxant responses to flunitrazepam (2 mg/kg, i.p.) and to sodium valproate (696 mg/kg, i.p.) was shown to depend upon mild warming of the animals with radiant heat, a procedure which can increase muscle spindle afferent input to the spinal cord. 7 The results suggest a hyperactivity of stretch reflexes in the spastic mouse, ameliorated selectively by those drugs that enhance the GABA-mediated presynaptic inhibition of such pathways.

Animals↗

Cerebral dopamine, apomorphine and oral activity in the neonatal pig.

Neonatal piglets in which oral stimulation associated with feeding was reduced by intragastric tube feeding displayed an increase in stereotyped snout rubbing, licking and chewing behaviour. An investigation of a possible neurochemical basis for this behaviour was made by using sensitive radioenzymatic and microfluorimetric assays to estimate the concentrations of the catecholamines and of the dopamine metabolites homovanillic acid (HVA) and 3,4-dihydroxyphenyl-acetic acid (DOPAC) in different brain regions. These observations revealed that the increased non-nutritive oral activity of such piglets did not appear to be caused by an increased release of dopamine in the brain, since it was not associated with increases in the concentrations of the acidic metabolites of dopamine in either the caudate nucleus, the putamen, the nucleus accumbens, the olfactory tubercle, the hypothalamus, or the substantia nigra. The only neurochemical changes observed were small decreases in the concentration of HVA in the putamen and the nucleus accumbens. A lack of effect on catecholamine concentrations in any of the six brain regions examined suggested that the environmental manipulation caused no changes in the development of catecholamine-containing nerve endings. Subcutaneous injection of apomorphine was found to increase the non-nutritive oral activity of piglets. Apparent conditioning effects of the environment on apomorphine-induced stereotyped behaviour however, prevented any satisfactory testing of possible changes in cerebral dopamine receptor sensitivity following reduced oral stimulation.

3,4-Dihydroxyphenylacetic Acid↗

Development of acute opioid tolerance and dependence in rat striatal neurones.

Striatal neurones in the rat were frequently observed to develop tachyphylaxis to the specific, naloxone-antagonisable depressant effects of methionine- and leucine-enkephalin on spontaneous and L-glutamate-evoked activity. This loss of responsiveness to the enkephalins occurred within a few minutes of the repeated or prolonged application of these peptides and is suggested to reflect a form of acute tolerance. As with chronic opiate tolerance, the acute tolerance of single striatal neurones to the enkephalins appeared to be associated with dependence on these opioids, as evinced by the withdrawal-like hyperactivity that occurred upon terminating the application of the peptides or upon the microelectrophoresis of naloxone.

Animals↗

A demonstration of naloxone-precipitated opiate withdrawal on single neurones in the morphine-tolerant/dependent rat brain.

1 A comparison has been made between the effects of microelectrophoretically applied naloxone on single neurones in the frontal cerebral cortex and the striatum of naive and of morphine-tolerant/dependent rats, anaesthetized with a mixture of alpha-chloralose and urethane. 2 Specificity of the results obtained was evaluated by contrasting the effects of alternate applications of the (+)- and (-)-isomers of naloxone to the same neurones. 3 In naive rats naloxone had predominantly no effect, only a few cells revealing non-specific depressant responses to the drug. 4 In morphine-tolerant/dependent rats a higher proportion of neurones responded to naloxone; either with stereospecific excitatory responses, in which the activity evoked by L-glutamate or acetylcholine was increased, or with a non-specific inhibition, similar to that observed in naive animals. 5 It is suggested that these excitatory responses to microelectrophoretically applied (-)-naloxone represent opiate withdrawal responses at the single neurone level and that they reflect a latent hyperexcitability of the postsynaptic membrane in the morphine-tolerant/dependent state.

Acetylcholine↗

Specific versus non-specific actions of opioids on hippocampal neurones in the rat brain.

An investigation has been made into the pharmacological specificity of the actions of microelectrophoretically applied opioids on neurones in the rat hippocampus, a structure containing a low concentration of specific receptors for these substances. The majority of hippocampal neurones remained unaffected by morphine or enkephalin. Some neurones, however, displayed either inhibitory or excitatory responses to the opioids. Of the inhibitory effects, a few appeared to be specific, in that they could be antagonized by naloxone, but most of the other inhibitory responses were found to be potentiated by this drug. Similarly, naloxone not only failed to antagonize, but frequently potentiated the excitatory responses to the opioids. Further evidence for the predominantly non-specific nature of the responses of hippocampal neurones to opioids was provided by experiments with the stereoisomers levorphanol and dextrorphan. Neurones could be found which were either inhibited or excited by both enantiomers. Stereospecific responses, when observed, were inhibitory. Although non-specific, the excitatory effects of enkephalin and morphine on hippocampal neurones were greatly reduced in morphine tolerant/dependent rats. Indeed, in the hippocampus of these animals, the opioids had predominantly inhibitory effects which were potentiated, not antagonized, by naloxone. It is concluded that the low concentration of opiate receptors in the rat hippocampus renders neurones within this structure sensitive to a variety of nonspecific opioid actions.

Action Potentials↗

Neuronal aspects of opiate dependence and tolerance in comparison to central depressants.

Some acute and chronic effects of opiates and of central depressants have been reviewed, in order that a comparison can be made between the actions of these drugs. Special emphasis has been given to opiate-induced changes at the neuronal level, which have been studied either by the direct microelectrophoretic application of drugs to single neurones or by application of drugs to the myenteric plexus/longitudinal muscle preparation of the guinea pig ileum. Available evidence suggests that chronic exposure of nervous tissue to opiates as well as to central depressants causes changes in neuronal excitability, which become apparent upon withdrawal of the drug. Although opiates and central depressants cause similar changes they appear to do so by different mechanisms. Such differences between the mode of action of opiates and central depressants may provide an explanation for the differing chronic effects of these drugs.

Animals↗