neurotransmission

VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.

ATP (Adenosine triphosphate) provides cellular energy, participates in overall energy balance, and maintains intracellular homeostasis. ATP can act as an extracellular signaling molecule through interactions with specific purinergic receptors to mediate a variety of processes including neurotransmission, inflammation, apoptosis, and bone remodeling.

Besipirdine (HP 749 free base) is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine reduces schedule-induced irritability and thirst and enhances cholinergic and adrenergic activity in the CNS in the rat. Besipirdine reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system.

Besipirdine hydrochloride is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine hydrochloride inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine hydrochloride reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system in rats.

Rovatirelin (S-0373) is a newly synthesized thyrotropin-releasing hormone (TRH) analog that ameliorates cytosine arabinoside-induced motor dysfunction in a rat model of spinal cerebellar degeneration via acetylcholine and dopamine neurotransmission.

Quinidine hydrochloride monohydrate is an optical isomer of quinine, extracted from the bark of the Cinchona tree and similar plant species. It prolongs cellular action potential and decreases automaticity. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.

Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.

N-Acetylneuraminic acid (Acide aceneuramique) is a nine-carbon sialic acid monosaccharide commonly found in glycoproteins on cell membranes and in glycolipids such as gangliosides in mammalian cells. Studies have shown that N-Acetylneuraminic acid is biologically useful for neurotransmission, leukocyte extravasation, viral or bacterial infections, and carbohydrate-protein recognition.

Citalopram (Lu 10-171 is an orally active, selective serotonin reuptake inhibitor (SSRI), a selective 5-hydroxytryptamine reuptake inhibitor, and a racemic mixture of the S(+)-enantiomer (Escitalopram) and the R(-)-enantiomer.Citalopram exhibits antidepressant activity and enhances serotonergic neurotransmission. It can be used to study Alzheimer's disease.

IDRA-21 is a positive AMPA receptor modulator.

Fipexide (Attentil, Vigilor), a psychoactive drug of the piperazine chemical class, was developed in Italy in 1983. It was served as a nootropic drug in France and Italy, mainly for the therapy of senile dementia, but is no longer in common use because of the occurrence of rare drug side-effects including hepatitis and fever.

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

Telcagepant (MK-0974) is an oral calcitonin gene-related peptide receptor (CGRP) antagonist that blocks CGRP receptors and reduces neurotransmission in the central nervous system and is used in the study of migraines and for pain relief.

N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor, mimicking its action with Ki values of 2.3 nM, 790 nM, and 43 nM for human A1, A2A, and A3 receptors, respectively. CPA is used to modulate cellular signaling, neurotransmission, and other biological processes.

Picrotin is an inhibitor of glycine receptors. Picrotin blocks α2 GlyR, α1 GlyR, and α3 GlyR and can be used in studies about neurotransmission.

Norfenfluramine hydrochloride ((±)-Norfenfluramine hydrochloride) is the primary metabolite of Fenfluramine, resulting from its N-dealkylation. It serves as a potent anorectic agent and can modulate serotonin neurotransmission. In addition, Norfenfluramine hydrochloride exhibits sedative effects following acute administration.

YY-23 is a selective NMDAR (containing GluN2C or GluN2D) inhibitor. By inhibiting NMDARs with GluN2D on GABAergic interneurons in the prefrontal cortex, YY-23 suppresses GABAergic neurotransmission and enhances excitatory transmission. YY-23 exhibits antidepressant activity and is useful for neurological disease research.

Centpropazine (CNPZ) is a non-selective antagonist of serotonin (5-HT1/5-HT2) and adrenergic (α1) receptors. It exhibits antidepressant effects by modulating monoamine neurotransmission, particularly by reducing the reuptake of serotonin and norepinephrine. Centpropazine holds potential for research in the treatment of depression.

MDAR IN-1 (Compound 5m) is a brain-penetrant acetylcholinesterase (AChE) inhibitor and an antagonist of the NMDAR receptor GluN1/GluN2B subtype. It effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR to reduce excitotoxicity. MDAR IN-1 shows potential for Alzheimer’s disease research.

XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1].

Ro 8-4304 hydrochloride, an NMDA receptor antagonist, is a potent chemical compound used in research and clinical settings for its ability to inhibit glutamate-mediated neurotransmission.

Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.