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
Papers
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TL;DR: The baculovirus/Sf9 system is suitable for the recombinant expression and functional analysis of kinin receptors though limitations of the system have to be considered.
Abstract: G protein-coupled receptors such as the receptors for bradykinin are present in low copy numbers in most natural cells. To overcome the problems associated with the analysis of these receptors at the protein level, we used highly efficient expression systems such as the baculovirus/insect cell system. However, the structural and functional statuses of recombinant receptors have often remained elusive. We have expressed the two types of human kinin receptors, B1 and B2, in Sf9 cells. Both receptors are found on the surface of infected cells where they display the same pharmacological profiles as their cognate receptors of native cells. The functional analysis of kinin receptors coupled to the intracellular signaling pathways of Sf9 cells revealed differential patterns of ligand-induced phosphorylation for the two kinin receptors. The B1 receptor failed to undergo ligand-induced phosphorylation. However the B2 receptor showed selective phosphorylation of a minor 38 kDa band and lack of phosphorylation of a dominant 33 kDa band, indicating that only a fraction of the receptor protein is functionally linked to the kinase pathway. A striking discrepancy between the number of binding sites and the amount of receptor protein per cell (molar ratio of 1:20 to 1:1000) indicated that a significant portion of kinin receptors is associated with the intracellular compartments of Sf9 cells. Pulse-chase and immunoprecipitation experiments demonstrated that the heterogeneity of recombinant receptors is not due to proteolytic processing but likely reflects incomplete or lacking N-glycosylation. We conclude that the baculovirus/Sf9 system is suitable for the recombinant expression and functional analysis of kinin receptors though limitations of the system have to be considered.
59 citations
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TL;DR: The data collectively suggest that AT1R/B2R heterodimerization does not occur as a natural consequence of their simultaneous expression in the same cell nor does the B2R influence the At1R signaling.
59 citations
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TL;DR: Cell-based functional assays are capable of the uHTS throughput required for chemical genomic research, and their functional nature provides distinct advantages over ligand-binding assays in the identification of target-selective modulators.
58 citations
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23 Dec 2002TL;DR: In this article, spiroazacyclic compounds were used as monoamine receptor modulators. And the following methods for identifying a subject suitable for treatment using said compounds were proposed: (1) inhibiting an activity of a monoamine receptors with said compounds; (2) treating a disease condition associated with a monoaminergic receptor using such compounds; and
Abstract: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
58 citations
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26 Sep 2005TL;DR: In this article, the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)N′-(4-(2-methylpropyloxy)-phenylmethyl) carbamide and its properties were presented.
Abstract: Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.
56 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 |