F
Fabrice Piu
Researcher at ACADIA Pharmaceuticals Inc.
Publications - 30
Citations - 698
Fabrice Piu is an academic researcher from ACADIA Pharmaceuticals Inc.. The author has contributed to research in topics: Receptor & Agonist. The author has an hindex of 16, co-authored 30 publications receiving 645 citations.
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Journal ArticleDOI
Pharmacological and Behavioral Profile of N-(4-Fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl) Carbamide (2R,3R)-Dihydroxybutanedioate (2:1) (ACP-103), a Novel 5-Hydroxytryptamine2A Receptor Inverse Agonist
Kimberly E. Vanover,David M. Weiner,Malath Makhay,Isaac Veinbergs,Luis R. Gardell,Jelveh Lameh,Andria L. Del Tredici,Fabrice Piu,Hans H. Schiffer,Thomas R. Ott,Ethan S. Burstein,Allan K. Uldam,Mikkel B. Thygesen,Nathalie Schlienger,Carl-Magnus A. Andersson,Thomas Son,Scott C. Harvey,Susan B. Powell,Mark A. Geyer,Bo-Ragner Tolf,Mark R. Brann,Robert E. Davis +21 more
TL;DR: ACP-103 is a potent, efficacious, orally active 5-HT2A receptor inverse agonist with a behavioral pharmacological profile consistent with utility as an antipsychotic agent and demonstrates >42.6% oral bioavailability in rats.
Journal ArticleDOI
Discovery of a Potent, Orally Available, and Isoform-Selective Retinoic Acid β2 Receptor Agonist
Birgitte W. Lund,Fabrice Piu,Natalie K Gauthier,Anne Eeg,Erika A. Currier,Vladimir Sherbukhin,Mark R. Brann,Uli Hacksell,Roger Olsson +8 more
TL;DR: Being an isoform-selective RARbeta2 receptor agonist that discriminates between nuclear receptor isoforms having identical ligand binding domains, 2 will be useful as a pharmacological research tool but also a valuable starting point for drug development.
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Identification of the first synthetic steroidogenic factor 1 inverse agonists: pharmacological modulation of steroidogenic enzymes.
Andria L. Del Tredici,Carsten B. Andersen,Erika A. Currier,Steven R. Ohrmund,Luke C. Fairbain,Birgitte W. Lund,Norman Nash,Roger Olsson,Fabrice Piu +8 more
TL;DR: 4-(heptyloxy)phenol (AC-45594), a prototype inverse agonist lead, was used to show that SF-1 constitutive activity can be pharmacologically modulated by a synthetic ligand.
Journal ArticleDOI
Broad modulation of neuropathic pain states by a selective estrogen receptor beta agonist.
Fabrice Piu,Cindy Cheevers,Lene Hyldtoft,Luis R. Gardell,Andria L. Del Tredici,Carsten B. Andersen,Luke C. Fairbairn,Birgitte W. Lund,Magnus Gustafsson,Hans H. Schiffer,John E. Donello,Roger Olsson,Daniel W. Gil,Mark R. Brann +13 more
TL;DR: ERb-131 a non-steroidal estrogen receptor beta ligand was evaluated in several pain animal models involving nerve injury or sensitization and demonstrated a critical effector in attenuating a broad range of anti-nociceptive states.
Journal ArticleDOI
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.
Hanna Pettersson,Anne Bulow,Fredrik Ek,Jacob Jensen,Lars Korsgaard Ottesen,Alma Fejzic,Jian Nong Ma,Andria L. Del Tredici,Erika A. Currier,Luis R. Gardell,Ali Tabatabaei,Darren Craig,Krista McFarland,Thomas R. Ott,Fabrice Piu,Ethan S. Burstein,Roger Olsson +16 more
TL;DR: A novel class of CB1 inverse agonists was discovered and a lead compound 11-(4-chlorophenyl)dibenzo[b,f][1,4]thiazepine-8-carboxylic acid butylamide (12e) which showed excellent in vivo activity in pharmacodynamic models related to CB1 receptor activity was discovered.