Structure-activity relationships of inverse agonists for G-protein-coupled receptors.
It has been recently established that G-protein-coupled receptors (GPCRs) can be constitutively active, i.e., they can be active in the absence of an agonist. This activity can be inhibited by so-called inverse agonists. For a number of GPCRs, such inverse agonists have been developed and studied, now enabling for the first time a study into their structure-activity relationships.
Soudijn
Willem
W
Leiden/Amsterdam Center for Drug Research, PO Box 9502, 2300RA Leiden, The Netherlands.
van Wijngaarden
Ineke
I
Ijzerman
Adriaan P
AP
D058907:Adenosine A1 Receptor Agonists; D058909:Adenosine A3 Receptor Agonists; D058646:Adrenergic alpha-1 Receptor Agonists; D058647:Adrenergic alpha-2 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000494:pharmacology; D000818:Animals; D063386:Cannabinoid Receptor Agonists; D018491:Dopamine Agonists / Q000494:pharmacology; D017442:Histamine Agonists / Q000494:pharmacology; D006801:Humans; D018721:Muscarinic Agonists / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology; D013329:Structure-Activity Relationship
D058907:Adenosine A1 Receptor Agonists; D058909:Adenosine A3 Receptor Agonists; D058646:Adrenergic alpha-1 Receptor Agonists; D058647:Adrenergic alpha-2 Receptor Agonists; D000318:Adrenergic beta-Agonists; D063386:Cannabinoid Receptor Agonists; D018491:Dopamine Agonists; D017442:Histamine Agonists; D018721:Muscarinic Agonists; D043562:Receptors, G-Protein-Coupled; D017366:Serotonin Receptor Agonists