Imetit dihydrobromide

Names

[ Name ]:
Imetit dihydrobromide

[Synonym ]:
Imetit dihydrobromide
S-[2-(Imidazol-4-yl)ethyl]isothiourea dihydrobromide

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[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.

Chemical & Physical Properties

[ Boiling Point ]:
430.8ºC at 760mmHg

[ Melting Point ]:
206 - 207 °C

[ Molecular Formula ]:
C₆H₁₂Br₂N₄S

[ Molecular Weight ]:
332.05900

[ Flash Point ]:
214.3ºC

[ Exact Mass ]:
329.91500

[ PSA ]:
103.85000

[ LogP ]:
3.29510

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933290090

Customs

[ HS Code ]: 2933290090

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist.

J. Pharmacol. Exp. Ther. 263 , 304, (1992)

The effects of a new agonist of histamine (HA) H3 receptors, Imetit (S-[2-(4-(imidazolyl)ethyl]isothiourea) were investigated in vitro and in vivo and compared to those of (R)-alpha-methylhistamine [(...