Design and discovery of a high affinity, selective and β-arrestin biased 5-HT7 receptor agonist
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DOI: 10.1007/s00044-021-02797-4
Abstract: Compound 1c, 5-chloro-2-(2-(3,4-dihydroisoquinolin-2(1H)-yl)ethyl)-2,3-dihydro-1H-inden-1-one was previously reported from our laboratory showing high affinity binding to the 5-HT7 receptor (Ki = 0.5 nM). However, compound 1c racemizes readily upon enantiomeric separation. To prevent racemization, we have redesigned and synthesized methyl… read more here.
Keywords: ht7 receptor; high affinity; arrestin biased;
Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT2A Receptor Agonists
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DOI: 10.1021/acs.jmedchem.2c00702
Abstract: The serotonin 2A receptor (5-HT2AR) is the mediator of the psychedelic effects of serotonergic psychedelics, which have shown promising results in clinical studies for several neuropsychiatric indications. The 5-HT2AR is able to signal through the… read more here.
Keywords: discovery arrestin; arrestin biased; biased 25cn; receptor ... See more keywords
Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling
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DOI: 10.1038/ncomms14335
Abstract: Acute hormone secretion triggered by G protein-coupled receptor (GPCR) activation underlies many fundamental physiological processes. GPCR signalling is negatively regulated by β-arrestins, adaptor molecules that also activate different intracellular signalling pathways. Here we reveal that… read more here.
Keywords: trpc3; acute catecholamine; secretion; catecholamine secretion ... See more keywords
Ang-(1-7) is an endogenous β-arrestin-biased agonist of the AT1 receptor with protective action in cardiac hypertrophy
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DOI: 10.1038/s41598-017-12074-3
Abstract: The renin-angiotensin system (RAS) plays a key role in the control of vasoconstriction as well as sodium and fluid retention mediated mainly by angiotensin (Ang) II acting at the AT1 receptor (AT1R). Ang-(1-7) is another… read more here.
Keywords: biased agonist; endogenous arrestin; hypertrophy; ang ... See more keywords
Distinct Mechanisms of β-Arrestin–Biased Agonist and Blocker of AT1R in Preventing Aortic Aneurysm and Associated Mortality
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DOI: 10.1161/hypertensionaha.122.19232
Abstract: Background: Aortic aneurysm (AA) is a “silent killer” human disease with no effective treatment. Although the therapeutic potential of various pharmacological agents have been evaluated, there are no reports of β-arrestin–biased AT1R (angiotensin-II type-1 receptor)… read more here.
Keywords: arrestin biased; trv027; mortality; blocker ... See more keywords