Affinity and efficacy of selective agonists and antagonists for vasopressin and oxytocin receptors: an "easy guide" to receptor pharmacology.
The development of "selective" drugs targeting oxytocin/vasopressin receptors has enormously progressed since the original synthesis of oxytocin more than 50 years ago. However, several factors still hamper the availability of a rich and complete range of selective agonists and antagonists acting at the different oxytocin/vasopressin receptor subtypes, making the use of these drugs still a daunting task. In this paper we will briefly review the major problems encountered when dealing with oxytocin/vasopressin selective ligands, proving few rules for their correct pharmacological use, in order to avoid common pitfalls. Finally, we will glimpse at new challenges, such us the discovery of coupling selective ligands, which foster the search for new classes of selective compounds.
Chini
Bice
B
CNR Institute of Neuroscience, Milan, Italy.
Manning
Maurice
M
Guillon
Gilles
G
D000818:Animals; D065092:Antidiuretic Hormone Receptor Antagonists; D002462:Cell Membrane / Q000187:drug effects / Q000502:physiology; D002468:Cell Physiological Phenomena; D007700:Kinetics; D008024:Ligands; D011485:Protein Binding; D018045:Receptors, Oxytocin / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000187:drug effects; D017483:Receptors, Vasopressin / Q000819:agonists* / Q000187:drug effects; D015290:Second Messenger Systems / Q000187:drug effects / Q000502:physiology; D013045:Species Specificity; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D065092:Antidiuretic Hormone Receptor Antagonists; D008024:Ligands; D018045:Receptors, Oxytocin; D017483:Receptors, Vasopressin