Synthesis of new 3-alkyl-6-arylhexahydropyrimidine-2,4-dione derivatives was achieved starting from various benzaldehydes. Their affinity towards the benzodiazepine receptor and their anticonvulsant effect were evaluated.

The syntheses of 1-substituted 3-ureidopropan-2-ols 2 and 3-acetyl-5-(1-phenyl-4-piperazinyl)methyl-2-oxazolidinones 5 from the corresponding 2-amino-2 oxazolines 1 are described. Some of these compounds have been investigated for psychotropic activity in mice using the skin conductance reaction (SCR)-habituation test. All the compounds produced a delay in habituation. The standard delaying dose (SDD 150) that delays SCR extinction until 150 100ths of an hour (+50% control time) was compared with that of the reference drug fenozolone for all the compounds.

1. The SCR-habituation test, used as a tool to detect an anxiolytic activity, is applied to the study of several anxiogenic drugs. This test is based on the measure of the SCR-extinction time (i.e. habituation) got by the way of an iterative photostimulus.2. 8 anxiogenic compounds are tested. They delay significantly and quantitatively the SCR habituation.3. Specificity, sensitivity and quantifying values of the test are considered in order to propose the use of the SCR-habituation test in the investigation of putative anxiogenic compounds.

Effective antihypoxic activity of new aminocyclopentanones which was higher than that of the reference compounds has been demonstrated by the SCR hypoxia test.

Cyclization of 2-(1-pyrrolyl)piperonylcarboxamide derivatives gave iminium perchlorates which afforded 9-(N-substituted-imino) and 9-(N-substituted amino)-6,7-methylenedioxypyrrolo[1,2-a]indoles.

La synthèse de nouveaux pyrrolo[1,2-a]indoles est décrite. Le test d'habituation révèle in vivo pour certains dérivés une activité psychostimulante non amphétaminique.

: Ibogane alkaloids were shown to have a very high arousal activity. Similarly, a stimulating CNS activity was demonstrated for vob-asine alkaloids. The influence of certain substituents was evidenced: a methoxy substituent increases the activity, while it is lowered by a methoxycarbonyl substituent.

1.1. Correlation between specific binding potencies “in vitro” of several benzodiazepines and activities in SCR-habituation test is very satisfactory.2.2. As the SCR-habituation test might be considered as an elementary model of anxiety state, the test is suggested to be used as an intermediate psychopharmacological tool before clinical study.3.3. SCR-magnitude test exhibits no correlation of this kind proving that sedative activity is of a different mechanism.

Anhidrotic concentrations 50 of four anticholinergics were determined in mice using an original skin palmar conductance method. Intra-peritoneal, intra-palmar and topical routes were compared. Relative anhidrotic activities according to the mode of administration of the different anticholinergics showed definite differences, e.g. hydroxyzine, which was the less active per i.p. route, was the most active per topical route. The method is likely to be a useful test for selecting the most active anticholinergic and its most efficient route of administration for the treatment of hyperhidrosis.