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| | IMETIT DIHYDROBROMIDE Basic information |
| Product Name: | IMETIT DIHYDROBROMIDE | | Synonyms: | S-[2-(IMIDAZOL-4-YL)ETHYL]ISOTHIOUREA DIHYDROBROMIDE;5-[2-(IMIDAZOL-4-YL)ETHYL]ISOTHIOUREA DIHYDROBROMIDE;IMETIT DIHYDROBROMIDE;IMETIT DIHYDROBROMIDE POTENT AND SELECTI VE;S-[2-(Imidazol-4-yl)ethyl]isothiourea2HBr;CarbaMiMidothioic acid, 2-(1H-iMidazol-4-yl)ethyl ester, dihydrobroMide;S-[2-(4(5)-Imidazolyl)ethyl]isothiourea dihydrobromide;SKF 91105 dihydrobromide | | CAS: | 32385-58-3 | | MF: | C6H12Br2N4S | | MW: | 332.06 | | EINECS: | | | Product Categories: | | | Mol File: | 32385-58-3.mol |  |
| | IMETIT DIHYDROBROMIDE Chemical Properties |
| storage temp. | Store at RT | | solubility | H2O: soluble | | form | solid | | color | off-white | | Water Solubility | Freely soluble in water, practically insoluble in acetone
/n | | InChI | 1S/C6H10N4S.2BrH/c7-6(8)11-2-1-5-3-9-4-10-5;;/h3-4H,1-2H2,(H3,7,8)(H,9,10);2*1H | | InChIKey | DOBOYMKCRRLTRF-UHFFFAOYSA-N | | SMILES | Br[H].Br[H].NC(=N)SCCc1c[nH]cn1 |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Eye Irrit. 2
Skin Irrit. 2
STOT SE 3 |
| | IMETIT DIHYDROBROMIDE Usage And Synthesis |
| Description | Imetit is a histamine H3 and H4 receptor agonist (Kis = 0.3 and 2.7 nM, respectively, in radioligand binding assays). It is selective for histamine H3 and H4 receptors over H1 and H2 receptors at concentrations up to 100 μM, as well as the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 240 nM)., Imetit reduces potassium-induced increases in histamine levels in isolated rat cerebral cortex slices (EC50 = 2.8 nM). It increases scratching in mice (ED50 = 0.9 μmol), an effect that is reduced by the H3 receptor antagonist thioperamide . | | Uses | Imetit dihydrobromide is a high affinity agonist at the histamine H3- and H4-receptors. | | Definition | ChEBI: A hydrobromide salt obtained by reaction of imetit with two equivalents of hydrobromic acid. An extremely potent, high affinity agonist at H3 and H4 receptors (Ki values are 0.3 and 2.7 nM respectively). Induces sh
pe change in eosinophils with an EC50 of 25 nM. Centrally active following systemic administration. | | Biological Activity | An extremely potent, high affinity agonist at H 3 and H 4 receptors (K i values are 0.3 and 2.7 nM respectively). Induces shape change in eosinophils with an EC 50 of 25 nM. Centrally active following systemic administration. Also available as part of the Histamine H 3 Receptor Tocriset™ . | | Biochem/physiol Actions | Potent and selective H3 histamine receptor agonist. | | storage | Store at RT | | References | [1] WILLIAM HOWSON . Two novel, potent and selective histamine H3 receptor agonists[J]. Bioorganic & Medicinal Chemistry Letters, 1992, 2 1: Pages 77-78. DOI: 10.1016/s0960-894x(00)80659-9
[2] ROB LEURS. Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed[J]. British Journal of Pharmacology, 1995, 116 4: 2315-2321. DOI: 10.1111/j.1476-5381.1995.tb15071.x
[3] M GARBARG. S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist.[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 263 1: 304-310.
[4] J K BELL J L R D S McQueen. Involvement of histamine H4 and H1 receptors in scratching induced by histamine receptor agonists in BalbC mice[J]. British Journal of Pharmacology, 2009, 142 2: 374-380. DOI: 10.1038/sj.bjp.0705754 |
| | IMETIT DIHYDROBROMIDE Preparation Products And Raw materials |
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