2. Academic Validation
  3. Discovery of heterocyclic nonacetamide synaptic vesicle protein 2A (SV2A) ligands with single-digit nanomolar potency: opening avenues towards the first SV2A positron emission tomography (PET) ligands

Discovery of heterocyclic nonacetamide synaptic vesicle protein 2A (SV2A) ligands with single-digit nanomolar potency: opening avenues towards the first SV2A positron emission tomography (PET) ligands

  • ChemMedChem. 2014 Apr;9(4):693-8. doi: 10.1002/cmdc.201300482.
Joël Mercier 1,  Laurence Archen,  Véronique Bollu,  Stéphane Carré,  Yves Evrard,  Eric Jnoff,  Benoît Kenda,  Bénédicte Lallemand,  Philippe Michel,  Florian Montel,  Florence Moureau,  Nathalie Price,  Yannick Quesnel,  Xavier Sauvage,  Anne Valade,  Laurent Provins
Affiliations

Affiliation

  • 1 Global Chemistry, UCB NewMedicines, UCB Pharma, Chemin du Foriest, B-1420 Braine-L'Alleud (Belgium). [email protected].
PMID: 24446373 DOI: 10.1002/cmdc.201300482
Abstract

The role of the synaptic vesicle protein 2A (SV2A) protein, target of the antiepileptic drug levetiracetam, is still mostly unknown. Considering its potential to provide in vivo functional insights into the role of SV2A in epileptic patients, the development of an SV2A positron emission tomography (PET) tracer has been undertaken. Using a 3D pharmacophore model based on close analogues of levetiracetam, we report the rationale design of three heterocyclic non-acetamide lead compounds, UCB-A, UCB-H and UCB-J, the first single-digit nanomolar SV2A ligands with suitable properties for development as PET tracers.

Keywords

epilepsy; imaging agents; levetiracetam; positron emission tomography (PET); synaptic vesicle proteins; tracers.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-136873
    99.96%, SV2A Radioligand