Chemical Name:N-[4-(1H-Imidazol-4-yl)butyl]-N'-methylthiourea oxalate
Biological Activity:
Histamine H3/H2 receptor
antagonist (Ki values are 0.07, 7.8 and 290 μM for H3,
H2 and H1 receptors respectively). Displays partial
agonist activity in SK-N-MC cells. Produces antinociceptive effects following
intraventricular administration (ED50 = 183 nmol/mouse in hot-plate
test).
Lambertiet
al (1996) Investigation into the role of histamine receptors in rodent
antinociception. Pharmacol.Biochem.Behav. 53 567. Houghet
al (2000) Antinociceptive activity of derivatives of improgran and
burimamide. Pharmacol.Biochem.Behav. 65 61.Wielandet
al (2001) Constitutive activity of histamine H3 receptors stably
expressed in SK-N-MC cells: display of agonism and inverse agonism by H3
antagonists. J.Pharmacol.Exp.Ther. 299 908.