Keynote review: histamine H3 receptor antagonists reach out for the clinic

S Celanire, M Wijtmans, P Talaga, R Leurs… - Drug discovery today, 2005 - Elsevier
Antagonists of the histamine H 1 and H 2 receptors have been successful as blockbuster
drugs for treating allergic conditions and gastric ulcers, respectively. As such, histamine …

Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression

…, S Poli, JM Vaugeois, EL Poul, S Celanire - Journal of …, 2011 - Taylor & Francis
There is growing evidence suggesting that antagonists of group II metabotropic glutamate
receptors (mGluR2/3) exhibit antidepressant-like properties in several preclinical models of …

Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders

…, ST Bate, IJ Reynolds, S Poli, S Celanire - … of Pharmacology and …, 2014 - ASPET
There is growing evidence that activation of metabotropic glutamate receptor 4 (mGlu 4 )
leads to anxiolytic- and antipsychotic-like efficacy in rodent models, yet its relevance to …

Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist

…, E Gelens, E Snip, RA Bakker, S Celanire… - Journal of medicinal …, 2004 - ACS Publications
In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic
pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at …

Recent advances in the drug discovery of metabotropic glutamate receptor 4 (mGluR4) activators for the treatment of CNS and non-CNS disorders

S Célanire, B Campo - Expert opinion on drug discovery, 2012 - Taylor & Francis
Introduction: The metabotropic glutamate receptor type 4 (mGluR4) plays a pivotal role in a
plethora of therapeutic areas, as recently demonstrated in preclinical validation studies with …

[HTML][HTML] Allosteric modulation of metabotropic glutamate receptor 4 activates IDO1-dependent, immunoregulatory signaling in dendritic cells

…, E Albini, R Bianchi, ML Belladonna, S Celanire… - …, 2016 - Elsevier
Metabotropic glutamate receptor 4 (mGluR4) possesses immune modulatory properties in
vivo, such that a positive allosteric modulator (PAM) of the receptor confers protection on mice …

[HTML][HTML] Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage

…, A Gaglione, B Riozzi, R Lütjens, SM Poli, S Celanire… - Molecular brain, 2015 - Springer
Background To examine whether metabotropic glutamate (mGlu) receptors have any role in
mechanisms that shape neuronal vulnerability to ischemic damage, we used the 4-vessel …

Base-assisted intramolecular 6-acetoxypyranone-acetylene [5+ 2] cycloaddition. Synthesis and reactivity of novel oxa-tricyclo [5.3. 1.01, 5] undecenones

S Celanire, F Marlin, JE Baldwin, RM Adlington - Tetrahedron, 2005 - Elsevier
The synthesis of 3,11-dioxatricyclo[5.3.1.0 ]undeca-5,9-dien-8-ones is reported from
suitable 5-substituted furfuryl alcohols bearing an acetylenic side-chain. Successive peracid-…

Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005–present)

S Celanire, I Sebhat, J Wichmann, S Mayer… - Expert Opinion on …, 2015 - Taylor & Francis
Introduction: This review focuses on the medicinal chemistry efforts directed toward the
identification of competitive and noncompetitive antagonists of glutamate at group II metabotropic …

[BOOK][B] Small molecule therapeutics for schizophrenia

S Celanire, S Poli - 2015 - Springer
Drug research requires interdisciplinary team-work at the interface between chemistry, biology
and medicine. Therefore, the new topic-related series Topics in Medicinal Chemistry will …