ZD7288

Product NameZD7288
CAS133059-99-1
MFC15H21ClN4
MW0
EINECS
MOL File133059-99-1.mol

Chemical Properties

storage temp.	Desiccate at +4°C
solubility	Soluble in DMSO
form	crystalline solid
color	White to off-white
Water Solubility	water: 100mM
InChI	1S/C15H20N4.ClH/c1-5-19(13-9-7-6-8-10-13)15-11-14(16-3)18(4)12(2)17-15;/h6-11H,5H2,1-4H3;1H
InChIKey	DUWKUHWHTPRMAP-UHFFFAOYSA-N
SMILES	Cl.[n]1([c](cc(nc1C)N(CC)c2ccccc2)=NC)C

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

ZD 7288 is a selective Ih channel inhibitor. ZD 7288 is an sino-atrial node function modulator; blocks the hyperpolarization activated cation current If. ZD 7288 blocks Ih in central neurons. ZD 7288 increases NMDA-evoked noradrenalin release in rat brain in vitro.

Biological Activity

Sino-atrial node function modulator; blocks the hyperpolarization activated cation current I f . Blocks I h in central neurons. Increases NMDA-evoked noradrenalin release in rat brain in vitro .

in vivo

Application of ZD7288 0.1 μM at 5 minutes before high-frequency stimulation significantly decreases the amplitude of field excitatory postsynaptic potentials (fEPSPs), and this inhibitory effect is maintained throughout the recording period. Application of 0.1 μM ZD7288 30 minutes after high-frequency stimulation almost completely reverses the established long-term potentiation (LTP). Following application of ZD7288 (0.1 μM) 5 minutes before high-frequency stimulation, glutamate content is reduced to 74.9±8.0% (P<0.05, vs. normal saline group). Furthermore, application of 0.1 μM ZD7288 30 minutes after high-frequency stimulation markedly decreases the glutamate content to 77.0%±9.4% (P<0.05, vs. normal saline group)^[1].

storage

Desiccate at +4°C

References

[1]. chen y, lin c, tang y, et al. zd 7288, an hcn channel blocker, attenuates chronic visceral pain in irritable bowel syndrome-like rats. world j gastroenterol, 2014, 20(8): 2091-2097.
[2]. sánchez-alonso jl, halliwell jv, colino a. zd 7288 inhibits t-type calcium current in rat hippocampal pyramidal cells. neurosci lett, 2008, 439(3): 275-280.
[3]. larkman pm, kelly js. modulation of the hyperpolarisation-activated current, ih, in rat facial motoneurones in vitro by zd-7288. neuropharmacology, 2001, 40(8): 1058-1072.
[4]. gasparini s, difrancesco d. action of the hyperpolarization-activated current (ih) blocker zd 7288 in hippocampal ca1 neurons. pflugers arch, 1997, 435(1): 99-106.

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