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
More filters
••
TL;DR: It was shown that structurally diverse ERβ-selective agonists also relieved allodynia in CINP caused by taxol, oxaliplatin, and vincristine, and it was confirmed that ER β-selectives have antiallodynic effects in the spinal nerve ligation model of neuropathic pain.
Abstract: Chemotherapy-induced neuropathic pain (CINP) remains a major unmet medical need. Estrogen receptor beta (ERβ)-selective agonists represent a novel strategy for treating CINP because they are neuroprotective and may also have anticancer activity. We confirmed that ERβ-selective agonists have antiallodynic effects in the spinal nerve ligation model of neuropathic pain. We then showed that structurally diverse ERβ-selective agonists also relieved allodynia in CINP caused by taxol, oxaliplatin, and vincristine. These effects were receptor subtype specific and mediated by ERβ receptors as ERα-selective and nonselective estrogen agonists were inactive, a mixture of an ERβ and ERα agonist was inactive, and ERβ-selective antagonists blocked the effects of the ERβ-selective agonists. The efficacy and potency of ERβ-agonists was greater in male rats than females. To address the possibility that AC-186 might stimulate proliferation of cancers, rendering it unsuitable for treating CINP, we evaluated proliferative eff...
14 citations
••
TL;DR: An improved synthetic route to the bicyclo[2.2]octane-2,6-diol ligands (2-6-BODOLS) allowed an increased structural variation of the ligand side-arm as mentioned in this paper.
Abstract: An improved synthetic route to the bicyclo[2.2.2]octane-2,6-diol ligands (2,6-BODOLS) allowed an increased structural variation of the ligand side-arm. The addition of aromatic or vinylic Grignard reagents to hydroxyketone 1 was highly selective and ligands 3f-3I were isolated in 84-97% yield. The addition of alkyl Grignard reagents containing beta-hydrogens resulted in lower yields (13-71%) due to competing ketone reduction. A number of 2,5-BODOLs were synthesized using a similar methodology. The ligands, together with Ti(OiPr)(4), were tested in the asymmetric reduction of acetophenone with catecholborane (up to 98% ee). 1-Naphthyl-BODOL 3i was employed as an allylboration reagent to benzaldehyde together with Sc(OTf)(3), resulting in (1S)-1-phenyl-3-buten-1-ol in 80% ee. (C) 2008 Elsevier Ltd. All rights reserved. (Less)
13 citations
••
TL;DR: A modified version of the Neurologic Evaluation Scale was administered to 80 patients with schizophrenia or schizoaffective disorder, once while on antipsychotic medications and once while off medication, utilizing cluster analysis and adding a medicated condition.
13 citations
•
16 May 2006TL;DR: In this article, an invention relates to compounds, their uses for the elucidation of PAR2 activity, and their use for the treatment or prevention of diseases or disorders related to PAR2 activities.
Abstract: This invention relates to compounds, their uses for the elucidation of PAR2 activity and their uses for the treatment or prevention of diseases or disorders related to PAR2 activity, wherein the compound has the general chemical structure:
13 citations
••
13 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 |