Effects of dimethylaminoethanol pyroglutamate (DMAE p-Glu) against memory deficits induced by scopolamine: evidence from preclinical and clinical studies.

Rationale: Dimethylaminoethanol pyroglutamate (DMAE p-Glu) is a compound resulting from the reaction between dimethylaminoethanol (an indirect precursor of acetylcholine) and pyroglutamic acid (a cyclic derivative of glutamic acid having procholinergic properties and promnesic effects in both animals and man).

Objectives: The present study undertook preclinical and clinical evaluations to test a potential therapeutic utility for DMAE p-Glu in cognitive impairments related to central cholinergic deficit.

Materials And Methods: In preclinical study, DMAE p-Glu was studied in rats by intracerebral microdialysis in conscious freely moving animals, on performance of rats in the Morris water maze test of spatial memory, and on the deficit in passive avoidance behavior induced by scopolamine.

Comedolytic effect of topical retinaldehyde in the rhino mouse model.

Background: Retinaldehyde is a key molecule in the metabolism of vitamin A by keratinocytes. In order to evaluate its range of topical activity in acne, its comedolytic effect was compared to that of retinoic acid in the same vehicle, in the rhino mouse model.

Methods: The animals were treated on the back daily for 5 consecutive days per week for 3 weeks.

[Diethyl benzylpiperazinomethyl and benzylpiperazinomethylbenzyl phosphonates as calcium inhibitors].

Two sets of phosphonic diethylester including a substituted benzylpiperazine moiety are synthesized. In spite of the spasmolytic or the calcium antagonistic potentialities of benzylpiperazine and phosphonic moieties, none of the six compounds, tested in vitro, exhibit any calcium antagonistic profile.

[The beta-adrenolytic activity of new arylmethyloxypropanolamine analogs of dioxadilol].

A series of arylmethyloxypropanolamines structurally related to Dioxadilol has been synthesized and tested for their beta adrenolytic activity. Only one compound, the benzofuranic derivative 3c, exhibited a similar activity as Dioxadilol but was less potent than propranolol.

Influence of the vinyl group on the calcium antagonistic activity of analogues of Fostedil.

Four aryl vinyl diethyl benzylphosphonates related to Fostedil were synthesized and evaluated for their in vitro calcium-inhibitory activity. None of these compounds exhibited any calcium antagonistic profile. Unlike a series of diethyl-styryl benzylphosphonates, previously described, the presence of two aromatic rings linked by a vinyl group did not improve the calcium antagonistic activity.