133059-99-1

Basic information

• Product Name: ZD7288
• Synonyms: N-ethyl-1,2-dimethyl-6-methylimino-N-phenyl-pyrimidin-4-amine hydrochl oride;ICI D2788;N-ethyl-1,6-dihydro-1,2-dimethyl-6-(methylimino)-N-phenyl-4-Pyrimidinamine hydrochloride;ICI D7288;N-Ethyl-1,6-dihydro-1,2-diMethyl-6-(MethyliMino)- N-phenyl-4-pyriMidinaMine Monohydrochloride
• CAS NO: 133059-99-1
• Molecular Formula: C15H21ClN4
• Molecular Weight: 292.807
• Product Categories: Ion Channels;Amines;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 133059-99-1.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 359.9°Cat760mmHg
• Flash Point: 171.4°C
• Appearance: /
• Density: g/cm³
• Vapor Pressure: 2.31E-05mmHg at 25°C
• Storage Temp.: Desiccate at +4°C
• Solubility: Soluble in DMSO
• CAS DataBase Reference: ZD7288(CAS DataBase Reference)
• NIST Chemistry Reference: ZD7288(133059-99-1)
• EPA Substance Registry System: ZD7288(133059-99-1)

Safety Data

• Hazardous Substances Data: 133059-99-1(Hazardous Substances Data)

Usage

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 .

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.

InChI:InChI=1/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/b16-14+;

Related news

A bradycardiac agent ZD7288 (cas 133059-99-1) blocks the hyperpolarization-activated current (Ih) in retinal rod photoreceptors09/10/2019

Recently it has been reported that “If channel blockers”, which block the hyperpolarization-activated inward current (If) in heart sino atrial node cells, also block the hyperpolarization-activated inward current (Ih) in other tissues. Here we compared the effects of one of these agents, ZD728...detailed

ZD7288 (cas 133059-99-1) inhibits exocytosis in an HCN-independent manner and downstream of voltage-gated calcium influx in pituitary lactotrophs☆09/09/2019

Pituitary lactotrophs fire action potentials spontaneously and the associated voltage-gated calcium influx is sufficient to maintain high prolactin release. Here we studied the role of hyperpolarization-activated cation channels in pacemaking activity, calcium signaling, and prolactin secretion ...detailed

The H current blocker ZD7288 (cas 133059-99-1) decreases epileptiform hyperexcitability in the rat neocortex by depressing synaptic transmission09/07/2019

Neurons respond to intracellular injection of hyperpolarizing current pulses by generating depolarizing sags contributed by a cation current termed Ih. Ih modulates neuron excitability and rhythmicity. It is, however, unclear whether the net effect of changing Ih leads to facilitation or depress...detailed

ZD7288 (cas 133059-99-1) inhibits low-threshold Ca2+ channel activity and regulates sperm function09/06/2019

In this study, ZD7288, a blocker of hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels, has been found to inhibit the mouse sperm acrosome reaction (AR). HCN channels have not yet been either recorded or implicated in mouse sperm AR, but low-threshold (T-type) Ca2+ channels h...detailed

Effects of ZD7288 (cas 133059-99-1) on firing pattern of thermosensitive neurons isolated from hypothalamus09/05/2019

The role of the hyperpolarization-activated current (Ih) mediated by HCN channels in temperature sensing by the hypothalamus was addressed. In warm-sensitive neurons (WSNs), exposure to ZD7288, an inhibitor of Ih mediated by hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, dec...detailed

Effects of tertiapin-Q and ZD7288 (cas 133059-99-1) on changes in sinoatrial pacemaker rhythm during vagal stimulation09/04/2019

Heart rate slowing produced by cardiac parasympathetic (vagal) stimulation is thought to be the result of modulation of the acetylcholine-activated K+ current (IK,ACh) and the pacemaker current (If) in sinoatrial (SAN) pacemaker cells. However, the contribution of these and other ion currents to...detailed

Research reportHCN channel antagonist ZD7288 (cas 133059-99-1) ameliorates neuropathic pain and associated depression09/02/2019

Chronic neuropathic pain has demonstrated that coexisting psychiatric disorders are associated with disability and poorer treatment outcomes. Hyperpolarization-activated cyclic nucleotide-gated (HCN, Ih) channels play a major role in pain via hyperexcitability and facilitation of ectopic firing ...detailed