administration

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

Antiulcer Agent 1 is an orally administered derivative of 2-(3,4-dimethoxyphenyl)ethylamine.

BD-AcAc 2 (Ketone Ester) is a ketone monoester and can be used as a source of oral nutritional ketones. BD-AcAc 2 can elevate plasma levels of acetoacetate and β-hydroxybutyrate, blood Na+, blood glucose levels and blood creatinine levels after oral administration in mice. BD-AcAc 2 can partly prevent muscle weakness in septic mice. BD-AcAc 2 exhibits potential to improve endurance and exercise performance in animal body. BD-AcAc 2 can also be used to research diabetes or Parkinson's disease.

Oxaquin is an effective, water-soluble, injectable prodrug that is rapidly converted to the active substance MCB3681 after intravenous administration in the body. Oxaquin is active against Gram-positive bacteria, but has no antibacterial effect on its own.

Epsilon-momfluorothrin (Momfluorothrin, (Z,1R,3R)-), a type I synthetic pyrethroid insecticide, exerts its insecticidal properties and triggers activation of the constitutive androstane receptor (CAR). Notably, its administration in rats has been observed to induce the development of hepatocellular tumors.

Etripamil (MSP-2017) displays atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells. Etripamil is an antagonist of short-acting L-type calcium-channel. It has a rapid onset of action designed for intranasal administration. It is also used to treat Paroxysmal Supraventricular Tachycardia.

Lecozotan HCl (SRA-333) is a potent and selective 5-HT antagonist that significantly enhances KCl-stimulated glutamate and acetylcholine release from the hippocampal dentate gyrus and has cognitive enhancing properties. Chronic administration of Lecozotan HCl did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model demonstrating 5-HT(1A) receptor function.

PGP-4008 is a selective and potent P-glycoprotein (Pgp) inhibitor that inhibits tumor growth by co-administration with Doxorubicin.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

Ciamexon (Ciamexone) is a novel immunomodulator that has shown promising results in experimental models of autoimmune disease with little demonstrated cytotoxicity.Ciamexon can be used to study endocrine ophthalmopathies and diabetes mellitus, with slight improvement in ophthalmic disease following short-term administration.

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2 M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).This compound is unstable in powder form and other related salt forms are recommended.

Potassium iodide is used as the treatment of overactive thyroid and as protection of the thyroid gland from the influences of radiation from swallowed or inhaled radioactive iodine. It may be used after accidental exposure to radioactive iodine or before and after administration of medicine containing radioactive iodine.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

Chloroxine (Capitrol) is a synthetic quinoline derivative with antibacterial activity. Although the mechanism of action is not fully understood, topical administration of chloroxine diminishes mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp, including psoriasis and eczema.

Terpin hydrate, a cis-form hydrate, is derived from sources such as oil of turpentine, oregano, thyme, and eucalyptus. It is used as an insect repellent and expectorant. Terpin hydrate(cis-Terpin hydrate) is commonly used to loosen mucus and ease congestion in patients presenting with acute or chronic bronchitis, and related pulmonary conditions. It was popular in the United States since the late nineteenth century, but was removed from marketed medications in the 1990s after the U.S. Food and Drug Administration (FDA) stated that based on the evidence currently available, there are inadequate data to establish general recognition of the safety and effectiveness of these ingredients . Elixirs of terpin hydrate are still available with a prescription but must be prepared by a compounding pharmacy.

3-Hydroxy-4-methoxyacetophenone (Acetoisovanillone) is an active P. spinosa extract. It possesses anti-inflammatory activity and prevented injuries due to administration of acetic acid in the colon.

Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.

Ketanserin (Ketanserinum) is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation.

Citicoline sodium (CDP-choline) is an endogenous intermediate in the synthesis of phosphatidylcholine. It also serves as a choline donor in the biosynthesis of the neurotransmitter acetylcholine. Citicoline sodium demonstrates protective effects in cerebral ischemia, traumatic brain injury, and memory disorders. Exogenous administration of citicoline to rodents (500 mg kg i.p. immediately after ischemia and at 3-h reperfusion) has been shown to stimulate the synthesis of phosphatidylcholine, sphingomyelin, and cardiolipin and to attenuate the release of arachidonic acid and the accumulation of ceramide.

Tropicamide (Ro 1-7683) is a synthetic muscarinic antagonist with anticholinergic properties similar to atropine. Upon ocular administration, it binds to and blocks muscarinic receptors in the sphincter and ciliary muscles, inhibiting cholinergic responses and causing pupil dilation and ciliary muscle paralysis. Tropicamide is used as a diagnostic agent to induce short-duration mydriasis and cycloplegia.

Phenazopyridine hydrochloride (Pyridium) is used orally as a urinary tract analgesic. Side effects of phenazopyridine hydrochloride administration can include nausea, interference with the oxygen-carrying capacity of red blood cells (methemoglobinemia), hemolytic anemia as well as renal and hepatic toxicity. It is reasonably anticipated to be a human carcinogen.