Tramiprosate, also known as homotaurine, is a gamma-Aminobutyric acid (GABA) receptor agonist and a glycosaminoglycan mimetic used in the treatment of Alzheimer's disease.

Pramoxine, also known as Pramocaine, is a topical anesthetic. Pramoxine decreases the permeability of the neuronal membrane to sodium ions by reversibly binding to and inhibiting voltage-gated sodium channels. This results in stabilization of the membrane and, thereby inhibiting the ionic fluxes required for membrane depolarization, hence resulting in the failure to initiate a propagated action potential and subsequent conduction blockade.

Phthalylsulfathiazole is a broad spectrum antimicrobial agent. Phthalylsulfathiazole is used in the treatment of dysentery, colitis, and gastroenteritis.

Phenoxybenzamine hydrochloride is an α-1 adrenergic receptor antagonist used to treat hypertension and as a peripheral vasodilator. Phenoxybenzamine reduced neuronal death in rat hippocampal slice cultures following exposure to oxygen glucose deprivation. Phenoxybenzamine treated TBI (traumatic brain injury) animals also showed a significant improvement in both learning and memory compared to saline treated controls. At 32 h post-TBI phenoxybenzamine treated animals had significantly lower expression of pro-inflammatory signaling proteins CCL2, IL1β, and MyD88, suggesting that phenoxybenzamine may exert a neuroprotective effect by reducing neuroinflammation after TBI.

Paromomycin sulfate is an aminoglycoside antimicrobial agent derived from Streptomyces sp. AG-P 1441. Paromomycin likely induced resistance as confirmed by the expression of pathogenesis-related genes: PR-1, β-1,3-glucanase, chitinase, PR-4, peroxidase, and PR-10, which enhanced plant defense against P. capsici in chili pepper.

Isoxsuprine is a beta 2-adrenergic agonist and NR2B subtype-selective N-methyl-D-aspartate (NMDA) receptor antagonist used for the treatment of pre-term labor and dysmenorrhea. Isoxsuprine affects the vascular smooth muscle and results in peripheral vascular dilation. Isoxsuprine also relaxes the uterine smooth muscles. Isoxsuprine elevated the blood flow volume in the umbilical arteries. Veterinary treatment of cows with isoxsuprine may temporarily lead to low levels of isoxsuprine in the hair of their newborn calves, which promotes growth.

Iodoquinol is one of the halogenated 8-quinolinols that's widely used as an intestinal antiseptic, especially as an antiamebic agent. Iodoquinol is also used topically in other infections and may cause central nervous system and eye damage.

Hematein, also known as Haematein, is an oxidized derivative of Hematoxylin (Haematoxylin) used in staining the staining of cell nuclei in animal tissue. Hematein also can be used in the staining of myelin sheaths and nerve fibers.

Ergoloid Mesylates, also known as dihydroergotoxine mesylate, is a mixture of three dihydrogenated ergot alkaloids (dihydroergocristine, dihydroergocornine, and alpha- and beta-dihydroergocryptine). Ergoloid mesylates is used as a treatment for dementia and Alzheimer disease. Ergoloid Mesylates stimulates dopaminergic and serotonergic receptors and blocks alpha-adrenoreceptors. Ergoloid Mesylates binds to the GABAA receptor Cl- channel, producing a reaction at the benzodiazepine site.

Domiphen bromide is a quaternary antiseptic used as an antifungal agent. Domiphen bromide has potent activity on blockade of human ether-a-go-go related gene (HERG) channels. Domiphen bromide inhibited HERG channel currents in a dose-dependent manner with IC50 values of 9nM. Block of HERG channel by domiphen bromide was voltage-dependent and use-dependent. Domiphen bromide caused substantial negative shift of the activation curves, accelerated activated process, but had no effects on the deactivation and reactivation processes.

Dehydrocholic acid is a semisynthetic bile acid synthesized from cholic acid. Dehydrocholic acid caused a dramatic decrease of phospholipid, cholesterol and bilirubin concentration but had little effect on bile acids concentration. Bile flow, expressed as the ratio of bile flow to bile acid excretion, was increased after dehydrocholic acid administration. It was speculated that the hydroxy keto metabolites are hydrocholeretics. The proportion of cholesterol to lecithin and bile acids did not change significantly after dehydrocholic acid administration.

Denatonium, also known as Bitrex, is a bitterant (or bitter agonist). Denatonium activates bitter taste receptors on many cell types and plays important roles in chemical release, ciliary beating and smooth muscle relaxation through intracellular Ca(2+)-dependent pathways. Denatonium significantly effects cellular morphology, decreases cell proliferation and reduces the number of cells in S phase in a dose-dependent manner. Denatonium causes large amplitude swelling of mitochondria, which was confirmed by the loss of mitochondrial membrane potential, the down-regulation of Bcl-2 protein and the subsequent enhancement of the mitochondrial release of cytochrome c and Smac/DIABLO after denatonium treatment.

Cinchonidine is an cinchona alkaloid with antimalarial activity. Cinchonidine adsorbed onto a platinum metal catalyst leads to rate acceleration and induces strong stereocontrol in the asymmetric hydrogenation of trifluoroacetophenone. In the hydrogenation of the heteroaromatic ring of cinchonidine in toluene, the diastereomeric excess of the (S)-hexahydrocinchonidine increased upon increasing Pt{111}/Pt{100} ratio, but this distinct shape selectivity was observed only after the oxidative removal of PAA at 473 K. The use of the as-prepared nanoparticles inverted the major diastereomer to R, and this isomer was formed also in acetic acid.

Chlortetracycline hydrochloride, also known as Aureomycin, is a broad-spectrum antibiotic used in veterinary medicine for pulmonary or digestive infections. Chlortetracycline and its metal complexes are toxic to bacteria when they are biologically available. Chlortetracycline and copper plus Chlortetracycline supplementation increased both the prevalence and gene copy numbers of tetA, while decreasing both the prevalence and gene copies of tetB.

Butamben, also known as Butoform, is a local anesthetic. Blockade of voltage-gated channel expressed in the peripheral sensory neurons has been suggested as a mechanism of action. Butaben effects on another sensory neuronal channel family, transient receptor potential (TRP) have remained unclear. Butamben attenuated acute animal pain behaviors in a TRPA1- or TRPV4-dependent manner. Butamben inhibits the total barium current through expressed calcium channel types in PC12 cells, including Cav1.2/L-type channels.

Bisacodyl, also known as Dulcolax, is a stimulant laxative drug. Oral bisacodyl is an effective and well-tolerated treatment for patients with chronic constipation. It improves bowel function, constipation-related symptoms, and disease-related quality of life.

Apomorphine Hydrochloride, also known as APL-130277 and TAK-251, is a dopamine D2 agonist used for the treatment of Parkinson's disease. Apomorphine also promotes intraneuronal amyloid-β (Aβ) degradation and improves memory function in an Alzheimer's disease model. Protein levels of two types of serine-phosphorylated insulin receptor substrate-1 (IRS-1), pS616 and pS636/639, significantly decreased following Apomorphine treatment in the 13-month-old 3xTg-AD mice brain, suggesting improved brain insulin resistance.

Anthralin, also known as Dithranol, is a hepsin activity inhibitor used for treatment of psoriasis Inhibition of hepsin activity suppresses the invasive growth of the tumor. Anthralin exerts a direct effect on keratinocytes and leukocytes. Anthralin significantly prolonged the prophase of mitotic keratinocytes in subtoxic doses and suppressed the expression of keratin 6 mRNA in the immediately suprabasal layer of psoriatic epidermis in vivo. Anthralin also inhibits the transformation of lymphocytes and the release of reactive oxygen species from activated leukocytes, in vitro.

CP-74006 is a selective D5D inhibitor. CP-74006 potently blocks the Delta5D activity with an IC(50) value of 20 nM and simplifies the metabolism of [1-(14)C]-alpha-linolenate (C18:3, cis-9,12,15) by accumulating (14)C-eicosatetraenoic acid (C20:4, cis-8,11,14,17) as the major (14)C-eicosatrienoic acid (C20:3, cis-11,14,17) and (14)C-docosatetraenoic acid (C22:4, cis-10,13,16,19) as the minor metabolites through Delta6 desaturation and elongation.

Atorvastatin lactone, also known as Atorvastatin Related Compound H, is a prodrug form of atorvastatin, an HMG-CoA reductase inhibitor used to lower blood cholesterol levels. It hydrolyzes rapidly to the acid form of atorvastatin in human serum.

PU-02 is a potent and selective 5-HT3 receptor antagonist. PU02 displays IC(50) values of ~1 μM at 5-HT(3)Rs and substantially lower activities at other Cys-loop receptors. In an elaborate mutagenesis study of the 5-HT(3)A receptor guided by a homology model, PU02 is demonstrated to act through a transmembrane intersubunit site situated in the upper three helical turns of TM2 and TM3 in the (+)-subunit and TM1 and TM2 in the (-)-subunit.

OXSI-2 is an Syk Inhibitor. OXSI-2 blocks nigericin-induced inflammasome signaling and pyroptosis independent of potassium efflux. OXSI-2 inhibits inflammasome assembly, caspase-1 activation, IL-1β processing and release, mitochondrial ROS generation, and pyroptotic cell death. Using a novel live cell potassium sensor we show that Syk inhibition with OXSI-2 has no effect on potassium efflux kinetics and that blockade of potassium efflux with extracellular potassium alters Syk phosphorylation.

AR-420626 is a FFA3 agonist. FFA3 is a promising target for the treatment of neurogenic diarrheal disorders by suppressing nAChR-mediated neural pathways.

TAN-420C, also known as Dihydroherbimycin C, is an antibiotic. TAN 420C is a minor analogue of the herbimycin complex, isolated from Streptomyces hygroscopicus. TAN 420C is known to exhibit antitumour activity.

GSK656, also known as GSK3036656 and GSK070, is a potent Mtb LeuRS inhibitor. GSK656 shows potent inhibition of Mtb LeuRS (IC50 = 0.20 μM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 μM). Additionally, it is highly selective for the Mtb LeuRS enzyme with IC50 of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. In addition, it exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads. GSK656 has been progressed to clinical development for the treatment of tuberculosis.

MDK-4111 is a potent and selective GPR120 receptor agonist. MDK-4111 has CAS#1234844-11-1. The last 4 digit of its CAS# is used for naming.

NF-1819 is a Potent and selective irreversible MAGL inhibitor.

PZ-II-029 is a α6β3γ2-selective GABAA channel modulator.

PF-04628935 is is a potent antagonist/inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. Ghrelin and GSHR are involved in regulation of food intake and long-term energy homeostasis; GSHR ligands are of interest for obesity and other metabolic disorders. PF-04628935 is orally bioavailable and brain penetrant.

ML-030, also known as CID-11757146, is a potent and selective PDE4 inhibitor. ML-030 inhibits PDE4 in a cell-based cyclic nucleotide-gated cation channel biosensor assay with an EC50 value of 18.7 nM.