Institution
ACADIA Pharmaceuticals Inc.
Company•San Diego, California, United States•
About: ACADIA Pharmaceuticals Inc. is a company organization based out in San Diego, California, United States. It is known for research contribution in the topics: Pimavanserin & Receptor. The organization has 260 authors who have published 276 publications receiving 8418 citations.
Papers published on a yearly basis
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TL;DR: In this article, a library of amides, synthesised by mixing acyl chlorides and diamines, was transformed into the corresponding thioamides using Lawesson's reagent as the oxygen/sulphur exchange reagent.
45 citations
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TL;DR: A novel cellular proliferation assay for examining signal transduction to Rap utilizing Ras–rap chimeras that respond selectively to Rap-specific exchange factors, but which stimulate cellular proliferation through Ras effectors indicates that GPCRs coupled to pertussis-toxin-sensitive G-proteins activate Rap through a Gα subunit, C3G, and Src-dependent pathway.
Abstract: Ras proteins mediate the proliferative effects of G-protein-coupled receptors (GPCRs), but the role of Rap proteins in GPCR signaling is unclear. We have developed a novel cellular proliferation assay for examining signal transduction to Rap utilizing Ras-rap chimeras that respond selectively to Rap-specific exchange factors, but which stimulate cellular proliferation through Ras effectors. Both the D1 dopamine receptor (Gs-coupled) and the 5HT1E serotonin receptor (Gi-coupled) mediated cellular proliferation in a Ras/rap chimera-dependent manner. Responses to both receptors were PKA-independent. Both receptors activated Ras/rap and full-length Rap as measured by activation-specific probes. Pertussis toxin blocked Ras/rap-dependent responses to 5HT1E but not D1. Ras/rap-dependent responses to both receptors were insensitive to beta-gamma scavengers. Responses to 5HT1E, but not D1, were sensitive to inhibition by a dominant-negative C3G fragment, by the Src-like kinase inhibitors PP1 and PP2, and by a dominant-negative mutant of Src. Very similar data were obtained for two other Gi-coupled receptors, the D2 dopamine receptor and the alpha2C adrenergic receptor. A constitutively active mutant of Galphai2 also mediated Ras/rap-dependent responses. These data indicate that GPCRs coupled to pertussis-toxin-sensitive G-proteins activate Rap through a Galpha subunit, C3G, and Src-dependent pathway.
43 citations
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TL;DR: The sequential addition of Grignard reagents and aldehydes or ketones to pyridine N-oxides yields a complete regio- and stereoselective trans 2,3-addition reaction in high yields, and the substituted 2, 3-dihydropyridineN-oxide can be reduced to form 2,4-trans-substituted piperidines.
Abstract: Reactivity N - Own: Pyridine N-oxides can be used for the complete regio- and stereoselective synthesis of trans-substituted piperidines. The sequential addition of Grignard reagents and aldehydes or ketones to pyridine N-oxides yields a complete regio- and stereoselective trans 2,3- addition reaction in high yields, and the substituted 2,3-dihydropyridine N-oxide can be reduced to form 2,3-trans-substituted piperidines (see scheme).
42 citations
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TL;DR: The discovery and characterization of two structurally different, potent, selective, and metabolically stable small-molecule PAR-2 agonists are presented, which may be useful as pharmacological tools for elucidating the complex physiological role of thePAR-2 receptors as well as for the development of PAR- 2 antagonists.
Abstract: 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, potent, selective, and metabolically stable small-molecule PAR-2 agonists. These ligands may be useful as pharmacological tools for elucidating the complex physiological role of the PAR-2 receptors as well as for the development of PAR-2 antagonists.
42 citations
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26 Sep 2005TL;DR: In this paper, the salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl), N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide of formula (I) including the citrate, fumarate, maleate, malate, phosphate, succinate, sulphate, and edisylate salts.
Abstract: Disclosed herein are salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide of formula (I) including the citrate, fumarate, maleate, malate, phosphate, succinate, sulphate, and edisylate salts.
42 citations
Authors
Showing all 261 results
Name | H-index | Papers | Citations |
---|---|---|---|
Michael Bachmann | 63 | 360 | 14388 |
Daniel P. van Kammen | 47 | 168 | 6957 |
Kristina Luthman | 39 | 158 | 7344 |
Fredrik Almqvist | 37 | 170 | 4219 |
Mark R. Brann | 35 | 77 | 5579 |
Roger Olsson | 30 | 138 | 2752 |
Uli Hacksell | 29 | 99 | 2954 |
Torbjörn Frejd | 29 | 165 | 2889 |
Petrine Wellendorph | 27 | 83 | 2573 |
Ethan S. Burstein | 27 | 70 | 2255 |
David M. Weiner | 26 | 45 | 3230 |
Kimberly E. Vanover | 25 | 70 | 1955 |
Uli Hacksell | 25 | 129 | 2879 |
Magnus Gustafsson | 25 | 94 | 1546 |
Mark R. Brann | 24 | 39 | 2576 |