Preparation and biological effects of pure stereoisomeric novel soft anticholinergics.

A series of pure stereoisomeric soft glycopyrrolate analogues 3, 4 and 5 was synthesized using chiral intermediates and by careful separation of the stereoisomers formed during the last quaternization step of the synthesis. The stereochemistry of the products was elucidated using various 1D and 2D NMR techniques. Anticholinergic activity of the new compounds was determined by receptor binding studies and performing tests on isolated organs and by in vivo tests.

New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox.

The present study examined the dose- and time-dependent central effects of an estradiol chemical delivery system cyclodextrin complex (E(2)-CDS-CD) on the reestablishment of copulatory behavior of castrated male and ovariectomized female rats with concomitant determination of the blood luteinizing hormone (LH) and E(2) levels. In orchidectomized males, Estredox, after single doses of 0.3 and 3.

Further evidence for the neuroleptic-like activity of gamma-endorphin.

gamma-Endorphin inhibits the amphetamine-induced stereotypy in rats with an approximate ED50 of 0.3 mg/kg. SC.