Title : Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor.

Pub. Date : 2014 Apr

PMID : 24476583






2 Functional Relationships(s)
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1 In this study we measured the phospholipid affinity and receptor binding kinetics of several clinically relevant beta2-adrenoceptor agonists and antagonists and demonstrated that the degree of phospholipid interaction directly affects the observed kinetic association rate (k on) and dissociation constant (Kd), but not the dissociation rate (k off) from the target, by concentrating drug in the local environment around the receptor. Phospholipids adrenoceptor beta 2 Homo sapiens
2 In this study we measured the phospholipid affinity and receptor binding kinetics of several clinically relevant beta2-adrenoceptor agonists and antagonists and demonstrated that the degree of phospholipid interaction directly affects the observed kinetic association rate (k on) and dissociation constant (Kd), but not the dissociation rate (k off) from the target, by concentrating drug in the local environment around the receptor. Phospholipids adrenoceptor beta 2 Homo sapiens