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P Chaillet

Publications and source records attributed to P Chaillet.

24 records · Page 2Linked to original sources

Inhibition of the spontaneous climbing behavior elicited in mice by opiates.

The spontaneous climbing behavior (SCB) developed by naive mice when they are introduced into small individual cylindrical cages with walls of vertical bars is inhibited in a dose-dependent manner by all the tested opiates. Only nalorphine administered over a large scale of doses never completely inhibits the SCB; its maximal effect is only about 50% of total inhibition. The efficacy of opiates on this special component of the locomotor activity has been compared with that on the horizontal displacements measured with an actometer equipped with photoelectric cells. Whereas the drugs known as specific kappa agonists depress both the horizontal locomotor activity and the SCB, most of the other tested opiates inhibit the SCB at doses which do not modify the horizontal locomotion. The low efficacy of loperamide, an opiate agent crossing the blood-brain barrier with difficulty, as well as the strong efficacy of a morphine low dose injected i.c.v. suggest that the opiate-induced SCB inhibition is centrally mediated. Finally, the involvement of mu and kappa receptors is discussed from the observed interactions with various opiate agonists, partial agonist (nalorphine) and antagonists (naloxone and diprenorphine).

Animals↗

Peptidases involved in the inactivation of exogenous and endogenous enkephalins.

Among the various cerebral enzyme activities able to hydrolyse the enkephalins into inactive fragments only two seem responsible for the metabolism of the endogenous opioid peptides: a dipeptidylcarboxypeptidase ("enkephalinase"), and a bestatin-sensitive aminopeptidase. Their inhibition by thiorphan and bestatin results in an antinociceptive effect observed in tests in which the nociceptive stimulation is probably accompanied by a concomittent release of enkephalins.

Aminopeptidases↗

Enkephalin metabolism in brain and its inhibition.

Various cerebral peptidases are able to hydrolyse the enkephalins into inactive fragments. Among these enzymes enkephalin-dipeptidylcarboxypeptidase ("enkephalinase") inhibited by thiorphan and a bestatin-sensitive aminopeptidase activity seem to play a key-role as "inactivating neuropeptidases". Their inhibition, in vitro as well as in vivo, leads to a protection of endogenous enkephalins and to antinociceptive effects.

Aminopeptidases↗

Simultaneous assessment of the opiate-induced modifications in the vertical and horizontal components of locomotor activity in mice.

The effects of some opiates on the horizontal and vertical components of locomotor activity in mice were measured in actometers fitted with photoelectric cells counting horizontal displacements and the striding over a low partition wall. Morphine and fentanyl, used at low doses which did not modify the horizontal locomotor activity, decreased the striding over of the partition wall. Such a dissociation was not observed with either kappa or sigma agonists which affected in the same way the two components of the locomotor activity: both components were inhibited by kappa agonists and slightly stimulated by the sigma agonist SKF 10047. Although the opiate-induced inhibition of the striding over was induced by low doses of morphine, relatively high doses of naloxone were necessary for its antagonism. This apparently difficult antagonism could result in fact from the sedation which appeared when morphine was associated with naloxone.

Animals↗