N-methyl-D-aspartate (NMDA) Receptor Screening Library

Rapid neurotransmission at excitatory glutamatergic synapses is mainly mediated by two types of postsynaptic glutamate receptors: α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) and NMDAR. The glutamate receptor of NMDA subtype is composed of two GluN1 and two GluN2 subunits, two obligatory NR1 subunits and two regionally localized NR2 subunits. Activation of NMDA receptors requires the binding of glutamate or aspartate. In addition, NMDAR requires binding of the antagonist glycine to effectively open the ion channel. The ability of glutamate and glycine or serine coagonists to continuously conduct Na⁺ and Ca²⁺ ions is due to their binding that can produce a slower and longer-lasting NMDAR openings. Currently, NMDA receptors have emerged as attractive therapeutic targets for the development of novel neuroprotective drugs. NMDA receptor antagonists are a class of anesthetics that act by competitively inhibiting the action of N-methyl-d aspartate receptors.

BOC Sciences has designed a novel N-methyl-d-aspartate nmda receptor screening library containing more than 1000 structurally diverse drug-like screening compounds of potential NMDA channel blockers.

Application of NMDA Receptor

• Acts as an important target for the development of neuroprotective drugs since it occupies a major position in the mechanism of ischemic brain injury
• Plays a crucial role in the etiology of ischemic stroke and some neurodegenerative diseases such as schizophrenia, Parkinson's disease, and Alzheimer's disease
• Treatment of schizophrenia and refractory depression

Figure 1. Proposed mechanism for NMDA receptor-mediated increases in cAMP in the striatum. (Nash, J. E.; Brotchie, J. M. 2000)

N-methyl-D-aspartate (NMDA) Receptor Screening Library Design

1. Firstly, BOC Sciences applies molecular docking strategy to select these compounds, and divides them into the following three subsets that are focused against each possible binding site:
• Competitive antagonists
• Glycine antagonists
• Noncompetitive antagonists
2. Finally, the resulting potential ion channel modifiers will be carefully filtered through the Rule of Five, PAINS and internal filters to remove molecules with undesired and reactive moieties

N-methyl-D-aspartate (NMDA) Receptor Screening Library Characteristics

• Favorable physicochemical parameters and solubility requirements
• No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
• Bioactivity and safety confirmed by preclinical studies and clinical trials
• Structural diversity, medicinal activity, and cellular penetration
• Structural document, IC₅₀, and other chemical and biological data are provided
• All compounds are continually updated
• Compound cherry-picking service is provided

What We Deliver

• Delivered within 2 weeks in any customer-preferred format
• Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
• All compounds have a minimum purity of 90% assessed by H NMR and HPLC
• ntagonist glycine to effectively open the ion channel. The ability of glutamate and glycine or serine coagonists to continuously conduct Na ⁺ and Ca ²⁺ i
• Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of N-methyl-D-aspartate (NMDA) Receptor Screening Library design at competitive prices for global customers. Personalized and customized services of N-methyl-D-aspartate (NMDA) Receptor Screening Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!