Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity...

type. Terms that describe this phenomenon are "functional selectivity", "protean agonism", or selective receptor modulators. As mentioned above, agonists...

animal studies. TCB-2 25C-NBOMe 25CN-NBOH – 100× selectivity for 5-HT2A over 5-HT2C, 46× selectivity over 5-HT2B. 3-Carboxy indole PB-22 (1-pentyl-indole-3-carboxylic...

consistent with the hypothesis that aripiprazole has "functionally selective" actions. The "functional-selectivity" hypothesis proposes that a mixture of agonist/partial...

selectivity, in pharmacology Functional selectivity, in pharmacology Natural selection, in biology Reactivity–selectivity principle, in general chemistry...

4-benzodiazepine. The functional selectivity is not unique to the nonbenzodiazepine structural class and has more to do with selectivity among different types...

This differential strategy has been given several names, including functional selectivity and biased agonism. The first opioid that was intentionally designed...

differences between AAS in terms of their intracellular metabolism, functional selectivity (differential recruitment of coactivators), and non-genomic mechanisms...

tools to synthesize functionalized aromatic compounds with high selectivity. The widely used approach to achieve ortho-selectivity involves metal-chelating...

the first demonstration of functional selectivity with dopamine receptors. Dinapsoline – full agonist with 5-fold selectivity for D1-like receptors over...

models with intermediate conformational states. The discovery of functional selectivity and that ligand-specific receptor conformations occur and can affect...

(2018-08-06). "Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity". International Journal of Neuropsychopharmacology. 21 (10): 962–977...

subtypes can transactivate transcription only when a heterodimer with the functional ERß1 receptor of 59 kDa is formed. The ERß3 receptor was detected at high...

in high selectivity based on innate substrate selectivity for a given reaction or based on catalyst control. The discovery of site-selective LSF reactions...

concentration that is required to stimulate the 2C receptors. This functional selectivity is critical to prevent potential side effects and suggests that...

chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand...

Functional agonist may refer to: functional selectivity Physiological agonism This disambiguation page lists articles associated with the title Functional...

assessed as H3 antagonist, later found to be an agonist, shows functional selectivity, activating some G-protein coupled pathways but not others) Imbutamine...

known as NLX-101, is a potent and selective 5-HT1A receptor full agonist. In addition, it displays functional selectivity, or biased agonism, by preferentially...

(COX-2), an enzyme responsible for inflammation and pain. Targeting selectivity for COX-2 reduces the risk of peptic ulceration and is the main feature...

that this might be due to its low intrinsic efficacy, rather than functional selectivity or 'G protein bias' as initially reported. In tests on mice, PZM21...

relies on xanomeline's functional selectivity for the M1 and M4 muscarinic receptors, with trospium chloride, a peripherally selective antimuscarinic added...

Hasenhuetl PS, Bhat S, Freissmuth M, Sandtner W (March 2019). "Functional Selectivity and Partial Efficacy at the Monoamine Transporters: A Unified Model...

Cariprazine Cannabidiol GSK-789,472 – Also D3 antagonist, with good selectivity over other receptors Ketamine (also NMDA antagonist) LSD – in vitro,...

lower doses are not well understood; however, it may be mediated by functional selectivity and/or preferentially binding to D2 autoreceptors at low doses,...

the μ-opioid receptor than mitragynine. These compounds display functional selectivity and do not activate the β-arrestin pathway partly responsible for...

agonists. 22-Thiocyanato-salvinorin A is notable because of its functional selectivity. 2-Methoxymethyl Salvinorin B is seven times more potent than Salvinorin...

~10-fold selectivity over 5-HT2A and 5-HT2C BW-723C86 – 100-fold selectivity over 5-HT2A but only 3- to 10-fold selectivity over 5-HT2C, fair functional subtype...

It is a selective agonist for the androgen receptor, producing functional selectivity with effective dissociation of anabolic and androgenic effects,...

led to the obtainment of new derivatives endowed with binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype. Wheeler,...