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.

Full Text
Paper version not known

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call

Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.