An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation.
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The analgesic efficacy of fentanyl: relationship to tolerance and mu-opioid receptor regulationGaddum Memorial Lecture 2014: receptors as an evolving concept: from switches to biased microprocessorsModeling cell signaling networksThe classification of peripheral 5-HT2-like receptors using tryptamine agonist and antagonist analoguesA simple method for quantifying functional selectivity and agonist biasA conserved motif in the membrane proximal C-terminal tail of human muscarinic m1 acetylcholine receptors affects plasma membrane expression.The recombinant 5-HT1A receptor: G protein coupling and signalling pathways.A three-parameter two-state model of receptor function that incorporates affinity, efficacy, and signal amplification.Buprenorphine/naloxone reduces the reinforcing and subjective effects of heroin in heroin-dependent volunteers.Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptorEstimation of competitive antagonist affinity from functional inhibition curves using the Gaddum, Schild and Cheng-Prusoff equations.Functional methods for quantifying agonists and antagonists.The simcyp population based simulator: architecture, implementation, and quality assurance.Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling.P2Y1-receptors in human platelets which are pharmacologically distinct from P2Y(ADP)-receptors.Molecular and pharmacological evidence for MT1 melatonin receptor subtype in the tail artery of juvenile Wistar rats.Functional role of muscarinic M(2) receptors in alpha,beta-methylene ATP induced, neurogenic contractions in guinea-pig ileum5-HT7 receptor efficacy distribution throughout the canine stomachSystems pharmacology approaches for optimization of antiangiogenic therapies: challenges and opportunities.A constitutively active mutant beta 2-adrenergic receptor is constitutively desensitized and phosphorylated.Characterization of acute homologous desensitization of mu-opioid receptor-induced currents in locus coeruleus neurones.Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and InternalizationFulfilling the Promise of "Biased" G Protein-Coupled Receptor Agonism.Opioid agonist efficacy predicts the magnitude of tolerance and the regulation of mu-opioid receptors and dynamin-2Receptor Reserve Moderates Mesolimbic Responses to Opioids in a Humanized Mouse Model of the OPRM1 A118G PolymorphismToward the prediction of CNS drug-effect profiles in physiological and pathological conditions using microdialysis and mechanism-based pharmacokinetic-pharmacodynamic modeling.A dileucine motif in the C terminus of the beta2-adrenergic receptor is involved in receptor internalization.Explaining the escalation of drug use in substance dependence: models and appropriate animal laboratory tests.Hydromorphone efficacy and treatment protocol impact on tolerance and mu-opioid receptor regulation.On the analysis of ligand-directed signaling at G protein-coupled receptors.Myocardial signaling defects and impaired cardiac function of a human beta 2-adrenergic receptor polymorphism expressed in transgenic mice.An estimation of beta 2-adrenoceptor reserve on human bronchial smooth muscle for some sympathomimetic bronchodilators.Application of a systems pharmacology model for translational prediction of hERG-mediated QTc prolongation.Minireview: More than just a hammer: ligand "bias" and pharmaceutical discovery.New concepts in pharmacological efficacy at 7TM receptors: IUPHAR review 2.Mechanistic analysis of the function of agonists and allosteric modulators: reconciling two-state and operational models.Quantitative analysis of receptor allosterism and its implication for drug discovery.The mass action equation in pharmacology.Signaling bias in drug discovery.
P2860
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P2860
An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation.
description
1985 nî lūn-bûn
@nan
1985年の論文
@ja
1985年論文
@yue
1985年論文
@zh-hant
1985年論文
@zh-hk
1985年論文
@zh-mo
1985年論文
@zh-tw
1985年论文
@wuu
1985年论文
@zh
1985年论文
@zh-cn
name
An operational model of pharma ...... sociation constant estimation.
@en
type
label
An operational model of pharma ...... sociation constant estimation.
@en
prefLabel
An operational model of pharma ...... sociation constant estimation.
@en
P2093
P2860
P1476
An operational model of pharma ...... sociation constant estimation.
@en
P2093
P2860
P304
P356
10.1111/J.1476-5381.1985.TB12941.X
P407
P577
1985-02-01T00:00:00Z