The present invention relates to a group of compounds which are xanthine derivatives and which act selectively at adenosine A1 receptors. Adenosine antagonists acting at the Al receptor depolarize postsynaptic neurons and presynaptically enhance the release of a number of neurotransmitters including acetylcholine, glutamate, serotonin, and norepinephrine. This action has potential for treating cognitive deficits such as those associated with Alzheimer's disease, as these transmitters have been implicated in learning and memory, and each of these transmitters is reduced in Alzheimer's disease. Some of the A1 antagonist compounds described in the present invention increased the activity of hippocampal neurons in a long-term potentiation in vitro learning model, and antagonized a scopolamine deficit in a water maze in vivo learning model. Thus, these compounds have potential for cognition-enhancing effects.
Xanthine Derivatives as Adenosine A1 Receptor Antagonists