sickness

Fexinidazole (HOE 239) is an antiparasitic agent with activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically relevant active metabolites in vivo are the sulfoxide and sulfone.

Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Acetazolamide sodium (OT-302 sodium) is a potent carbonic anhydrase (CA)IX inhibitor with diuretic, antigonococcal, and antihypertensive activity and may be used for indications such as epilepsy, glaucoma, edema, and altitude sickness.

Benzylamine hydrochloride, made of benzylamine and hydrochloric acid, is used to treat motion sickness and ascariasis, with antiemesis properties.

Alimemazine hemitartrate (Trimeprazine hemitartrate) is aphenothiazine derivative that is used as an antipruritic. It also acts as a sedative, hypnotic, and antiemetic for prevention of motion sickness.

Eflornithine (DFMO) is a selective and orally available ornithine decarboxylase inhibitor that delays hair overgrowth.Eflornithine is used in the study of African trypanosomiasis, malignant glioma, and sleeping sickness.

Zolamide (CL 5343) may be used to prevent altitude sickness and reduce the symptoms.

Pafuramidine (DB289) is an experimental prodrug of the orally active metabolite DB75, a potent antiparasitic compound with anti-malarial activity used in the study of parasitic infections and sleeping sickness.

Poskine is an anticholinergic and central nervous system depressant. It is utilized in research related to Parkinson's disease and motion sickness.

Scopolamine hydrobromide is a tropane alkaloid derived from the Solanaceae family. It is a high-affinity (nanomolar level) muscarinic receptor antagonist and can also reversibly inhibit 5-HT₃ receptor responses (IC₅₀ = 2.09 μM). It is commonly used to induce animal models of Alzheimer's disease or memory impairment.

Megazol is a nitroimidazole based drug that cures some protozoan infections. A study of nitroimidazoles found the drug extremely effective against T. cruzi and T. brucei which cause Chagas disease and African sleeping sickness, respectively.

O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killingTrypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50of less than 1 μM in a cell culture assay.1,2The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface glycoprotein (VSG), a protein critical for evading the host immune response.1O-11 exhibits essentially no anti-fungal activity when assayed usingC. neoformans, but does have a minor inhibitory effect on HIV-1 replication in T-lymphocytes.3 1.Doering, T.L., Raper, J., Buxbaum, L.U., et al.An analog of myristic acid with selective toxicity for African trypanosomesScience2521851-1854(1991) 2.Doering, T.L., Lu, T., Werbovetz, K.A., et al.Toxicity of myristic acid analogs toward African trypanosomesProceedings of the National Academy of Sciences of the United States of America919735-9739(1994) 3.Langner, C.A., Lodge, J.K., Travis, S.J., et al.4-Oxatetradecanoic acid is fungicidal for Cryptococcus neoformans and inhibits replication of human immunodeficiency virus IThe Journal of Biological Chemisty267(24)17159-17169(1992)

Vitamin B6 is a component of some coenzymes in human body, which is involved in a variety of metabolic reactions, especially related to amino acid metabolism.Clinical application of vitamin B6 in the prevention and treatment of pregnancy and radiation sic

Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.

hCAI II-IN-2 (compound 2b) is a highly effective dual inhibitor of human carbonic anhydrase I and II (hCA I II), with Ki values of 40.97 nM for hCA I, 15.15 nM for hCA II, and 61.88 nM for hCA IX. With its anti-hypoxic properties, hCAI II-IN-2 demonstrates activity against acute mountain sickness (AMS) and exhibits low cellular activity [1].

hCAI II-IN-4 (compound 6d) is a potent inhibitor of both hCA I and hCA II enzymes, with Ki values of 16.95 nM and 15.22 nM, respectively. It also inhibits hCA IX with a Ki value of 27.04 nM, exhibits anti-hypoxia properties, and maintains low toxicity. This compound is suitable for investigating acute mountain sickness (AMS) in research studies [1].

hCAI II-IN-3 (compound 5b) is a highly effective dual inhibitor of hCA I II enzymes, exhibiting Ki values of 51.25, 13.15, and 42.18 nM for hCA I, hCA II, and hCA Ⅸ, respectively. It demonstrates anti-hypoxic properties against acute mountain sickness (AMS) and exhibits low cellular activity [1].

Cinnarizine clofibrate is a calcium channel protein inhibitor as well as an antihistamine channel blocker. The compound is a drug derivative of piperazine. Cinnarizine is used for the control of vomiting due to motion sickness. It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus

NEU-1953 is a potential candidate for sleeping sickness.

5-Hydroxytryptophol is a metabolite of tryptophan. It is used as a biomarker for recent alcohol consumption and causes sleeping sickness