A1 adenosine receptors and their ligands:
overview and recent developments
by
Muller CE.
University of Bonn,
Pharmaceutical Institute,
Department of Pharmaceutical Chemistry, Germany.
christa.mueller@uni-bonn.de
Farmaco 2001 Jan-Feb; 56(1-2):77-80

ABSTRACT

Potent adenosine receptor (AR) agonists and antagonists with high selectivity for the A1AR subtype have been developed during the past decades. However, some of the compounds considered to be selective may not be as selective in humans as in rats, and may not be very selective versus the new AR subtypes A3 or A2B. Partial agonists have been developed that may exhibit fewer side effects than full agonists. Low water solubility of many A1 antagonists remains a problem. A1 AR antagonists can be classified as neutral antagonists or inverse agonists; the pharmacological consequences of inverse agonism versus neutral antagonism will have to be the subject of future investigations. Some medicinal plants (e.g. Hypericum perforatum and Valeriana officinalis) contain compounds that are antagonists or partial agonists at A1 ARs; effects on ARs may contribute to their pharmacological activity. 18F- and 11C-labeled A1 AR antagonists have been developed for positron emission tomography studies.

Coffee
Caffeine
Valerian
Adrafinil
Modafinil
Pemoline
Zopiclone
Insomnia
Adenosine
Amphetamine
St John's wort
Coffee and fags
Methylphenidate
Adenosine and reward
Hypersomnia and depression
Adenosine receptor antagonists
MAO inhibition in human coffee drinkers
Adenosine A(2A) receptors and depression

Refs
and further reading

HOME
HedWeb
Nootropics
cocaine.wiki
Future Opioids
BLTC Research
MDMA/Ecstasy
Superhapiness?
Utopian Surgery?
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World

The Good Drug Guide
The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family