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: Systemic administration showed that selective NPFF2 agonists are active in various pain models in vivo, whereas administration of a nonselective NPFF1 and NPff2 agonist increases sensitivity to noxious and non-noxious stimuli.
Abstract: We report the discovery and initial characterization of a novel class of selective NPFF2 agonists. HTS screening using R-SAT, a whole cell based functional assay, identified a class of aryliminoguanidines as NPFF1 and NPFF2 ligands. Subsequent optimization led to molecules exhibiting selective NPFF2 agonistic activity. Systemic administration showed that selective NPFF2 agonists (1 and 3) are active in various pain models in vivo, whereas administration of a nonselective NPFF1 and NPFF2 agonist (9) increases sensitivity to noxious and non-noxious stimuli.
29 citations
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TL;DR: Treatment of adults with DS with ELND005 at both doses was well tolerated, achieved measurable blood levels and demonstrated no safety findings, and further studies will be needed to test efficacy.
Abstract: Author(s): Rafii, Michael S; Skotko, Brian G; McDonough, Mary Ellen; Pulsifer, Margaret; Evans, Casey; Doran, Eric; Muranevici, Gabriela; Kesslak, Patrick; Abushakra, Susan; Lott, Ira T | Abstract: ELND005 (scyllo-Inositol; cyclohexane-1,2,3,4,5,6-hexol) has been evaluated as a potential disease-modifying treatment for Alzheimer's disease (AD). Individuals with Down syndrome (DS) have an increased risk for developing AD dementia.To evaluate the safety and tolerability of ELND005 and to determine its pharmacokinetics (PK) and relationship between PK parameters, safety outcome measures, and exploratory efficacy outcome measures in young adults with DS without dementia.This was a prospective, randomized, double-blind, placebo-controlled, parallel-group, three-arm, multicenter Phase II study of the safety and pharmacokinetics of ELND005 administered orally for 4 weeks (ClinicalTrials.gov NCT01791725). Participants who met study eligibility criteria were randomly assigned in a 2 : 1:1 ratio to receive ELND005 at either 250 mg twice daily (BID) or 250 mg once daily (QD) or matching placebo for 4 weeks.There were no apparent treatment group-related trends on cognitive or behavioral measures and there were no SAEs and no deaths in the study. Overall, mean changes from baseline in clinical laboratory parameters, vital sign measurements, electrocardiogram results, and other physical findings were unremarkable. ELND005 accumulation averaged approximately 2-fold with QD dosing, and 3- to 4-fold with BID dosing.Overall, treatment of adults with DS with ELND005 at both doses was well tolerated, achieved measurable blood levels and demonstrated no safety findings. Further studies will be needed to test efficacy.
29 citations
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TL;DR: In male rats, 17β-estradiol, which activates ERβ and ERα with equal potency, did not show the same neuroprotective benefits as AC-186, so in addition to a beneficial safety profile for use in both males and females, a selective ERβ agonist has a differentiated pharmacological profile compared to 17 β-ESTradiol in males.
Abstract: Drugs that selectively activate estrogen receptor β (ERβ) are potentially safer than the nonselective estrogens currently used in hormonal replacement treatments that activate both ERβ and ERα. The selective ERβ agonist AC-186 was evaluated in a rat model of Parkinson’s disease induced through bilateral 6-hydroxydopamine lesions of the substantia nigra. In this model, AC-186 prevented motor, cognitive, and sensorimotor gating deficits and mitigated the loss of dopamine neurons in the substantia nigra, in males, but not in females. Furthermore, in male rats, 17β-estradiol, which activates ERβ and ERα with equal potency, did not show the same neuroprotective benefits as AC-186. Hence, in addition to a beneficial safety profile for use in both males and females, a selective ERβ agonist has a differentiated pharmacological profile compared to 17β-estradiol in males.
29 citations
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TL;DR: A combinatorial scaffolding procedure for the synthesis and spatial arrangement of tripartite structures was developed and showed good results on both the horizontal and the vertical axes.
29 citations
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06 Mar 2001TL;DR: In this paper, a compound and methods for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect is provided for the use of formula (II).
Abstract: Compound and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound of formula (II) is administered to a patient in need of such treatment.
28 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 |