The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century,
yet recent data have revealed that many ligands can differentially activate signaling …

The past decade has witnessed a significant growth in the identification of allosteric
modulators of G protein–coupled receptors (GPCRs), ie, ligands that interact with binding …

α-Neurotoxins have been isolated from hydrophid, elapid and, more recently, colubrid snake
venoms. Also referred to as postsynaptic neurotoxins or 'curare mimetic'neurotoxins, they …

We have characterized desloratadine (5H-benzo [5, 6] cyclohepta [1, 2-b] pyridine, 8-chloro-
6, 11-dihydro-11-(4-piperidinylidene), CAS 100643-71-8) as a potent antagonist of the …

Snake venoms consist of a multitude of pharmacologically active components used for the
capture of prey. Neurotoxins are particularly important in this regard, producing paralysis of …

Novel isoxazolopyridone derivatives that are metabotropic glutamate receptor (mGluR) 7
antagonists were discovered and pharmacologically characterized. 5-Methyl-3, 6 …

Calcium is a key intracellular signal that controls manifold cellular processes over a wide
temporal range. The development of calcium‐sensitive fluorescent dyes and proteins …

The histamine H1-receptor (H1R) is an important mediator of allergy and inflammation. H1R
antagonists have particular clinical utility in allergic rhinitis and urticaria. Here we have …

Drug–receptor interactions are traditionally quantified in terms of affinity and efficacy, but
there is increasing awareness that the drug-on-receptor residence time also affects clinical …

The analysis framework used to quantify drug potency in vitro (eg, K d or K i) was initially
developed for classical pharmacology bioassays, for example, organ bath experiments …