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Neurotransmitter Transporter Inhibitors Library

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ChemDiv’s library of small molecules inhibiting the functional activity of neurotransmitter transporter proteins contains 10,813 compounds.

Neurotransmitter transporters are a group of specialized proteins primarily located in the membranes of neurons and glial cells that are critically important in the regulation of synaptic neurotransmission. Their main function is to provide the removal of neurotransmitter molecules from the synaptic cleft back into the presynaptic membrane or into surrounding glial cells. This process is essential for terminating synaptic transmission and recycling neurotransmitters for subsequent release. This reuptake mechanism is critical for maintaining the balance and proper functioning of the whole nervous system. The main types of neurotransmitter transporters include serotonin transporters (SERT), norepinephrine transporters (NET), dopamine transporters (DAT), and glutamate transporters, each corresponding to specific neurotransmitters: serotonin, norepinephrine, dopamine, and glutamate, respectively. These transporters are used as targets for various pharmacological agents, serving as inhibitors of SERT, NET, and DAT, which are widely used in the treatment of psychiatric and neurological disorders, such as depression and anxiety, because they increase neurotransmitter availability in the synaptic cleft. Glutamate transporters, on the other hand, play a key role in preventing excitotoxicity and are researched for their implications in neurodegenerative diseases.

Our library of neurotransmitter transporter inhibitors presents a valuable tool for drug discovery, particularly for developing therapies for neurological and psychiatric disorders. By selectively inhibiting the reuptake of key neurotransmitters like serotonin, norepinephrine, dopamine, and glutamate, these agents modulate synaptic neurotransmitter levels, enhancing or prolonging their action in the brain. This mechanism is fundamental in addressing conditions such as depression, anxiety, ADHD, and certain neurodegenerative diseases.

Our library offers a diverse range of inhibitors, each targeting specific transporters, thus allowing researchers to explore and identify compounds with optimal efficacy and safety profiles. Furthermore, the library facilitates the investigation of the various aspects of physiological mechanisms affected by those transporters involved in various disease states, potentially leading to the discovery of novel therapeutic targets. Our library may serve as a comprehensive resource for developing new drugs that could significantly improve the management and treatment of a variety of challenging mental health and neurological conditions.

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