SB-228357 was originally developed by scientists at Smith Kline Beecham (now merged with Glaxo Welcome to form GlaxoSmithKline). SB-228357 was identified as an antagonist of the serotonin receptors 5-HT2a/b/c with the highest affinity exhibited towards the 5-HT2C receptor. SB-228357 was identified for preclinical development as a treatment for depression, anxiety, and cataplexy but has not progressed beyond animal trials.

LY2033298 is a selective allosteric modulator for muscarinic acetylcholine M4 receptor. It exerts antipsychotic action in animal models. The compound is able to modulate circadian activity rhythms and morphine-induced conditioned place preference in rats.

SB-206606 (better known as BRL-37344) was developed by Beecham Pharmaceuticals and is currently licensable from GlaxoSmithKline. SB-206606 is an agonist for the Beta-3 adrenergic receptor with an EC 50 value of 17 nM (human B3AR expressed in CHO cells). SB-206606 was in pre-clinical development as a potential treatment of Diabetes Mellitus, although such efforts have been discontinued. Recently it has also garnered some interest as a potential treatment for alcoholism.

SKF-83822 is a D1/D5 receptor agonist, which activates D1-like receptors coupled to stimulation of adenyl cyclase (AC), but not phosphoinositide (PI) hydrolysis. SKF-83822 is used as a tool compound to study the role of AC-coupled D1 receptors.

Phenthiazamine was developed by Sekizawa et al. as a centrally acting anesthetic for fish. The time required to reduce the positive ganglionic potential in the sympathetic ganglion by phenthiazamine was prolonged in the presence of higher concentrations of Ca2+. The Ca2+-dependent action potential of guinea-pig ureter was reduced by this compound, whereas it did not affect the Na+-dependent action potential.

(-)-vesamicol is an active enantiomer of vesamicol (AH5183 or [(-)-trans-2-(4-phenylpiperidino)cyclohexanol]). It inhibits the uptake of acetylcholine into cholinergic neuronal storage vesicles. Vesicular acetylcholine transporter (VAChT) is inhibited by (-)-vesamicol, which binds tightly to an allosteric site.

AstraZeneca was developing the thiazole AR-AO-14418, a selective inhibitor of glycogen synthase kinase 3β (GSK-3β), for the treatment of Alzheimer's disease and major depressive disorder. AR-AO-14418 is an important research tool in as much as, at concentrations that AR-AO-14418 is able to inhibit GSK3 activity, this compound did not affect the activity of other 26 protein kinases tested, and especially does not inhibit cdc2 and cdk5, two GSK3-related kinases that are inhibited by published GSK3 inhibitors. Furthermore, AR-AO-14418 constitutes a lead compound with therapeutic potential for the treatment of AD, as well as other neurodegenerative disorders. Later preclinical studies of AR-AO-14418 were discontinued.

Sunifiram (DM235) is a piperazine derived research chemical which has anti-amnesiac effects in animal studies. Though Sunifiram is a piracetam derivative, it has a different chemical structure from the racetams and is chemically classed as a piperazine alkaloid. It is known to work in two ways, both as an ampakine that stimulates the activity of glutamine receptors and as a cholinergic that increases the production and release of acetylcholine. Like many nootropics, Sunifiram’s precise mechanisms of action are not entirely understood. However, it is believed that its primary action is that of an ampakine, which means that after crossing the blood-brain barrier it binds to AMPA-type glutamate receptors in the brain. This stimulates the production of glutamate, a vital neurotransmitter that plays the pivotal role in neural activation. Sunifiram is also thought to act as a cholinergic, increasing the production and release of the neurotransmitter acetylcholine. Though the exact process by which this occurs has not been identified, an Italian animal study showed that tests using piperazine compounds such as Sunifiram had a cholinergic effect similar to that of piracetam. No serious side effects of Sunifiram have been documented, but it’s important to remember that no human studies or clinical trials have been conducted.

BRL-54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. BRL-54443 (3-300 ug/paw) significantly reduced formalin-induced flinching in rats, indicating that it could be used as a therapeutic strategy to reduce inflammatory pain..

Potassium hydrogen DL-aspartate has being shown to inhibit cell damage and apoptosis induced by ouabain and H2O2. Principal neurotransmitter for fast synaptic excitation. DL-Aspartic acid (DL-Asp) is a racemic mixture of the proteinogenic amino acid L-aspartate and the non-proteinogenic amino acid D-aspartate. DL-Aspartic acid is used in studies on factors and conditions that enhance semen and sperm quality. DL-Aspartic acid is used to develop and assess amino acid racemic resolution and racemic interconversion technologies. Principal neurotransmitter for fast synaptic excitation. It has being shown that DL-Aspartic acid (DL-Asp) administration improves sperm quality in bucks and the high D-Asp content in seminal plasma suggests a primary role for this D-amino acid in regulatory mechanisms of reproductive activity.