Clobenpropit Dihydrobromide and it’s analogues functions as potent histamine H3 antagonist.
ChEBI: A hydrobromide salt obtained by reaction of clobenpropit with two equivalents of hydrobromic acid. An extremely potent histamine H3 antagonist/inverse agonist (pA2 = 9.93). Also displays partial agonist activity at
H4 receptors; induces eosinophil shape change with an EC50 of 3 nM.
The combination treatment of Clobenpropit (every other day intraperitoneal injection at 20 μM per kilogram for 40 d) and Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d) shows significant tumor growth inhibition[3].
| Animal Model: | Five-week-old male BALB/c nude mice with Panc-1 xenograft[3] |
| Dosage: | 20 μM per kilogram |
| Administration: | Intraperitoneal injection; every other day for 40 days. Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d) |
| Result: | The combination treatment showed significant tumor growth inhibition compared with other treatment groups (control 501±92 mg, Gemcitabine 294±46 mg, Clobenpropit 444±167 mg, and combination 154±54 mg). |
Human H3LR: 9.44 (pKi); Rat H3LR: 9.75 (pKi); H4 receptor: 13 nM (Ki); H2 Receptor: 5.6 (pKi)
![N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea Structure](/CAS/GIF/145231-35-2.gif)
