Cas No.: | 32385-58-3 |
Chemical Name: | Carbamimidothioic acid,2-(1H-imidazol-5-yl)ethyl ester, hydrobromide (1:2) |
Synonyms: | Carbamimidothioic acid,2-(1H-imidazol-5-yl)ethyl ester, hydrobromide (1:2);IMETIT DIHYDROBROMIDE;S-[2-(Imidazol-4-yl)ethyl]isothiourea dihydrobromide;S-[2-(4(5)-Imidazolyl)ethyl]isothiourea dihydrobromide;Carbamimidothioic acid, 2-(1H-imidazol-4-yl)ethyl ester dihydrobromide |
SMILES: | Br.Br.NC(SCCC1=CN=CN1)=N |
Formula: | C6H12Br2N4S |
M.Wt: | 332.059277534485 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with Ki values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC50=25 nM)[1][2][3]. |
Target: | H3 Receptor:0.3 nM (Ki) H4 receptor:2.7 nM (Ki) |
In Vivo: | Imetit dihydrobromide (2.5-10 mg/kg; i.p.) reduces the licking response induced by Apomorphine[4]. Animal Model: Male Sprague-Dawley rats[4] Dosage: 2.5, 5, 10 mg/kg Administration: i.p. (30 min before Apomorphine) Result: Reduced the licking response induced by Apomorphine. |
References: | [1]. Liu C, et al. Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6. [2]. Ling P, et al. Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol. 2004 May;142(1):161-71. [3]. Garbarg M, et al. S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist. J Pharmacol Exp Ther. 1992 Oct;263(1):304-10. [4]. Farzin D, et al. Influence of different histamine receptor agonists and antagonists on apomorphine-induced licking behavior in rat. Eur J Pharmacol. 2000 Sep 15;404(1-2):169-74. |