Functional selectivity and classical concepts of quantitative pharmacology
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 …
yet recent data have revealed that many ligands can differentially activate signaling …
Allosteric modulation of G protein–coupled receptors
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 …
modulators of G protein–coupled receptors (GPCRs), ie, ligands that interact with binding …
Alpha neurotoxins
CM Barber, GK Isbister, WC Hodgson - Toxicon, 2013 - Elsevier
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 …
venoms. Also referred to as postsynaptic neurotoxins or 'curare mimetic'neurotoxins, they …
Biochemical characterization of desloratadine, a potent antagonist of the human histamine H1 receptor
JC Anthes, H Gilchrest, C Richard, S Eckel… - European journal of …, 2002 - Elsevier
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 …
6, 11-dihydro-11-(4-piperidinylidene), CAS 100643-71-8) as a potent antagonist of the …
In vitro neuromuscular activity of snake venoms
WC Hodgson, JC Wickramaratna - Clinical and Experimental …, 2002 - Wiley Online Library
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 …
capture of prey. Neurotoxins are particularly important in this regard, producing paralysis of …
In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists
G Suzuki, N Tsukamoto, H Fushiki, A Kawagishi… - … of Pharmacology and …, 2007 - ASPET
Novel isoxazolopyridone derivatives that are metabotropic glutamate receptor (mGluR) 7
antagonists were discovered and pharmacologically characterized. 5-Methyl-3, 6 …
antagonists were discovered and pharmacologically characterized. 5-Methyl-3, 6 …
Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays
SJ Charlton, G Vauquelin - British journal of pharmacology, 2010 - Wiley Online Library
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 …
temporal range. The development of calcium‐sensitive fluorescent dyes and proteins …
[HTML][HTML] Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells
LA Stoddart, AJ Vernall, M Bouzo-Lorenzo, R Bosma… - Scientific reports, 2018 - nature.com
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 …
antagonists have particular clinical utility in allergic rhinitis and urticaria. Here we have …
Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism
G Vauquelin, S Bostoen, P Vanderheyden… - Naunyn-Schmiedeberg's …, 2012 - Springer
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 …
there is increasing awareness that the drug-on-receptor residence time also affects clinical …
The problems of applying classical pharmacology analysis to modern in vitro drug discovery assays: Slow binding kinetics and high target concentration
SRJ Hoare - SLAS DISCOVERY: Advancing the Science of …, 2021 - journals.sagepub.com
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 …
developed for classical pharmacology bioassays, for example, organ bath experiments …