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Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase.
TLDR
The hypothesis that DHX causes agonist-typical functional changes only at some of these receptors, termed "functional selectivity", suggests that drugs may be targeted not only at specific receptor isoforms but also at separate functions mediated by a single isoform, yielding novel approaches to drug discovery.
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(+)-6,7-Benzomorphan sigma ligands stimulate dopamine synthesis in rat corpus striatum tissue
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Inhibition of NADH oxidation by pyridine derivatives.
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Effects of polychlorinated biphenyls (PCBs) on brain tyrosine hydroxylase activity and dopamine synthesis in rats.
TLDR
The PCB-induced inhibition of tyrosine hydroxylase activity in mammalian forebrain observed here appears to occur through indirect and as yet unknown mechanisms.
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GPCR proteomics: Mass spectrometric and functional analysis of histamine H1 receptor after baculovirus‐driven and in vitro cell free expression
TLDR
The first successful use of MS analysis is reported to directly reveal the primary structure of hH1R protein, obtained from cell free and/or baculovirus expression system, and allows for further study the protein‐ligand interaction, by covalently labeling of the hH 1R protein with irreversible histaminergic compounds.
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Intracerebral microdialysis neurotoxicity studies of quinoline and isoquinoline derivatives related to MPTP/MPP+
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Ligand-Directed Functional Heterogeneity of Histamine H1 Receptors: Novel Dual-Function Ligands Selectively Activate and Block H1-Mediated Phospholipase C and Adenylyl Cyclase Signaling
TLDR
Results suggest the trans-PAT and cis-PAB probes will be useful to study molecular mechanisms of ligand-directed GPCR multifunctional signaling and provide a mechanistic basis for exploiting H1 receptor activation for drug design purposes.
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An Orally Active Phenylaminotetralin-Chemotype Serotonin 5-HT7 and 5-HT1A Receptor Partial Agonist that Corrects Motor Stereotypy in Mouse Models.
TLDR
Systemic (+)-5-FPT potently and efficaciously reduced or eliminated stereotypy in each of the mouse models without altering locomotor behavior on its own, and additional tests showed that (+)-2-fluorophenyl, at the highest behaviorally active dose tested, enhanced social interaction and did not cause behaviors indicative of serotonin syndrome.
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A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
TLDR
It is concluded that (-)-trans-H(2)-PAT is an antagonist at H(1) receptors coupled to PLC/IP formation and smooth muscle contraction and there may be post-translational H( 1) receptor heterogeneity.
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2-Phenylaminoadenosine stimulates dopamine synthesis in rat forebrain in vitro and in vivo via adenosine A2 receptors
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