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Intrinsic Efficacy of Antipsychotics at Human D2, D3, and D4 Dopamine Receptors: Identification of the Clozapine Metabolite N-Desmethylclozapine as a D2/D3 Partial Agonist
Drugs that antagonize D2-like receptors are effective antipsychotics, but the debilitating movement disorder side effects associated with these drugs cannot be dissociated from dopamine receptorExpand
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Discovery of potent and selective small-molecule PAR-2 agonists.
Proteinase activated receptor-2 plays a crucial role in a wide variety of conditions with a strong inflammatory component. We present the discovery and characterization of two structurally different,Expand
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Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor beta ligands.
We recently discovered the isoform selective RAR beta 2 ligand 4'-octyl-4-biphenylcarboxylic acid (3, AC-55649). Although 3 is highly potent at RAR beta 2 and displays excellent selectivity,Expand
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Pharmacology and Signaling Properties of Epidermal Growth Factor Receptor Isoforms Studied by Bioluminescence Resonance Energy Transfer
We have developed a new assay for measuring epidermal growth factor receptor (EGFR) activation using the bioluminescence resonance energy transfer (BRET) technology, which directly measures theExpand
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Identification and Characterization of Novel Small-Molecule Protease-Activated Receptor 2 Agonists
We report the first small-molecule protease-activated receptor (PAR) 2 agonists, AC-55541Expand
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Identification of the Atypical L-Type Ca2+ Channel Blocker Diltiazem and Its Metabolites As Ghrelin Receptor Agonists
Using a high-throughput functional screen, the atypical L-type Ca2+ channel blocker diltiazem was discovered to be an agonist at the human ghrelin (GHSR1a) receptor. In cellular proliferation, Ca2+Expand
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Identification of novel selective V2 receptor non-peptide agonists.
Peptides with agonist activity at the vasopressin V(2) receptor are used clinically to treat fluid homeostasis disorders such as polyuria and central diabetes insipidus. Of these peptides, the mostExpand
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Funcational assay platform to identify novel inhibitors of receptor tyrosine kinases
3144 Background: ACADIA has developed a functional assay to detect Receptor Tyrosine Kinase (RTK) activity, using its unique proprietary platform technology Receptor and Selection AmplificationExpand
Composes modulant par2 et leur utilisation
La presente invention porte sur des composes de formule chimique (I) et sur leurs utilisations, ou sur un sel acceptable d'un point de vue pharmaceutique de ceux-ci ou sur un promedicament deExpand
Identification and characterization of novel small molecule Protease Activated Receptor 2 ( PAR 2 ) agonists
243 words Introduction: 708 words Discussion: 1137 words