We have previously synthesized a series of hybrid compounds by linking ferulic acid to tacrine as multifunctional agents based on the hypotheses that Alzheimer's disease (AD) generates cholinergic deficiency and oxidative stress. Interestingly, we found that they may have potential pharmacological activities for treating AD. Here we report for the first time that tacrine-6-ferulic acid (T6FA), ...

Objective : This study was designed to examine the effects of orally administered Prunus persica water extract (PPE), which is used as herbal medicine, for treatment of Yu Xue (stasis of blood) and tacrine on the basal concentration of extracellular acetylcholine in the hippocampus of rats. Methods : To investigate the effects of PPE and tacrine on concentration of extracellular acetylcholine i...

A facile synthesis of potential acetylcholinesterase (AChE) inhibitors, the tacrine analogues 3a-p, has been accomplished by direct cyclocondensation of 1-aryl-4-cyano-5-aminopyrazole with β-ketoesters using tin(IV) chloride as catalyst. The structures of all the compounds have been confirmed by IR, ¹H- and ¹³C-NMR.

It has been demonstrated previously on the radial maze that the emergence of an age-related mnemonic impairment is critically dependent on the form which the discrimination problems took. Hence, when the arms were presented one by one (i.e., successive go-no-go discrimination), both adult and aged mice learned to distinguish between positive (baited) and negative (unbaited) arms readily, as evi...

OBJECTIVES The study was planned to determine cholinergic influence on different stages of memory - acquisition, consolidation and recall in scopolamine-induced amnesia (memory impairment) in mice. MATERIALS AND METHODS To study acquision, consolidation and recall stages of memory, we administered scopolamine (0.75, 1.5 and 3 mg/kg ip) 30 minutes and five minutes prior to first trial acquisit...

Inhibitors of the enzyme acetylcholinesterase (AChE) slow and sometimes reverse the cognitive decline experienced by individuals with Alzheimer's disease. Huperzine A, a natural product used in traditional Chinese herbal medicine, and tacrine (Cognex) are among the potent AChE inhibitors used in this treatment, but the search for more selective inhibitors continues. We report herein the synthes...

Transdermal iontophoresis is a method where the movement of ionic drugs (and sometimes also neutral drug molecules) across skin is enhanced using an externally applied potential difference. Iontophoretic devices contain three distinct components; 1) the drug reservoir which contains one electrode, the polarity chosen depends on the charge of the drug, 2) the return electrode and 3) the electron...