神经元信号相关配体
Effective neural communication is essential for all aspects of the nervous system's operation, spanning from its role in development and throughout the entire lifespan, including health and disease. Investigation of neuronal signaling pathways is essential for advancing our understanding of brain function, identifying the mechanisms underlying neurological and psychiatric disorders, and developing effective treatments and therapies.
Neurotransmitter receptors are mainly divided into ionotropic and metabotropic. Ionotropic indicates that ions can pass through the receptor, whereas metabotropic indicates that a second messenger inside the cell passes the message. Several kinds of metabotropic receptors, such as G protein-coupled receptors (including 5-HT receptor, histamine receptor, opioid receptor, etc.) as well as various ionotropic receptors (ligand-gated ion channels) are important therapeutic targets in neuronal signaling. Notch signaling also impacts to central nervous system including regulating neural stem cell proliferation, survival, self-renewal, and differentiation.
Neuronal Signaling Related Ligands Library contains 1727 small ligands, some representative molecules are given below: Acetylcholine (associated with Alzheimer's disease and myasthenia gravis), Gabapentin (epilepsy and seizures), Dopamine (Parkinson's disease) and Serotonin (depression).
Related terms: GPCR, ligand-gated IC, voltage-gated IC, catecholamine turnover, acetylcholine turnover, SLC6 neurotransmitter transporter family, GABA, CAMK, NAK
Mechanism of action of ionotropic(at left) and metabotropic(at right) neurotransmitter receptors (created by BioRender.com)
Highlights
Acetylcholine chloride, potent cholinergic agonist
Dopamine, a neurotransmitter
Serotonin, an endogenous agonist at 5-HT receptors
Gabapentin, analogue of γ-aminobutyric acid
Product Features
A set of 1727 molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target all major pharmaceutically relevant neuronal signaling targets.
Neuronal Signaling Related Ligands Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.86.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficient values, types of action on target and references to original literature.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.
Product Details
Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.
Utility
High throughput screening (HTS);
High content screening (HCS);
Cherry picking.