ZD 7288

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Cat.No. 1000 - ZD 7288 | C15H21ClN4 | CAS No. 133059-99-1
Description: Inhibits pacemaker (If) current
Alternative Names: ICI D7288
Chemical Name: 4-Ethylphenylamino-1,2-dimethyl-6-methylaminopyrimidinium chloride
Purity: ≥99% (HPLC)
Datasheet
Citations (30)
Literature

Biological Activity

Sino-atrial node function modulator; blocks the hyperpolarization activated cation current If (HCN channel). Blocks Ih in central neurons. Increases NMDA-evoked noradrenalin release in rat brain in vitro.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Compound Libraries

ZD 7288 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 292.81
Formula C15H21ClN4
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 133059-99-1
PubChem ID 123983
InChI Key DUWKUHWHTPRMAP-UHFFFAOYSA-N
Smiles [Cl-].CCN(C1=CC=CC=C1)C1=CC(NC)=[N+](C)C(C)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 29.28 100
water 29.28 100

Preparing Stock Solutions

The following data is based on the product molecular weight 292.81. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.42 mL 17.08 mL 34.15 mL
5 mM 0.68 mL 3.42 mL 6.83 mL
10 mM 0.34 mL 1.71 mL 3.42 mL
50 mM 0.07 mL 0.34 mL 0.68 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

BoSmith et al (1993) Inhibitory actions of ZENECA ZD7288 on whole cell hyperpolarization activated inward current (If) in guinea-pig dissociated sinoatrial node cells. Br.J.Pharmacol. 110 343 PMID: 7693281

Green et al (1996) Pharmacological characterization of the inwardly rectifying current in the smooth muscle cells of the rat bladder. Br.J.Pharmacol. 119 1509 PMID: 8982495

Harris and Constanti (1995) Mechanism of block by ZD7288 of the hyperpolarization-activated inward rectifying current in guinea-pig substantia nigra neurons in vitro. J.Neurophysiol. 74 2366 PMID: 8747199

Klar et al (2003) Ih channels as modulators of presynaptic terminal function: ZD7288 increases NMDA-evoked [3H]-noradrenaline release in rat neocortex slices. Naunyn Schmiedebergs Arch.Pharmacol. 367 422 PMID: 12690435


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Keywords: Sino-atrial node function modulators If inhibitors inhibits Channel VDAC ZD7288 ICID7288 AstraZeneca HCN ICI D7288 HCN Channels

30 Citations for ZD 7288

Citations are publications that use Tocris products. Selected citations for ZD 7288 include:

Ghezzi  et al (2016) Electrophysiological characterization of the M-current in rat hypoglossal motoneurons Neuroscience 340 62 PMID: 27984184

Asteriti et al (2015) A Cambrian origin for vertebrate rods. Elife 4 PMID: 26095697

Kashyap et al (2015) Characterization of the role of HCN channels in β3-adrenoceptor mediated rat bladder relaxation. Front Cell Neurosci 2 PMID: 26709376

Ferreira et al (2015) Highly differentiated cellular and circuit properties of infralimbic pyramidal neurons projecting to the periaqueductal gray and amygdala. PLoS One 9 161 PMID: 25972785

Ohno et al (2015) Hcn1 is a tremorgenic genetic component in a rat model of essential tremor. J Neurosci 10 e0123529 PMID: 25970616

Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol. J Neurophysiol 10 e0132884 PMID: 26222156

Williams and Hablitz (2015) Differential modulation of repetitive firing and synchronous network activity in neocortical interneurons by inhibition of A-type K(+) channels and Ih. Front Cell Neurosci 9 89 PMID: 25852481

Calejo et al (2014) Hyperpolarization-activated cyclic nucleotide-gated channels and cAMP-dependent modulation of exocytosis in cultured rat lactotrophs. J Neurosci 34 15638 PMID: 25411492

Dragicevic et al (2014) Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra dopamine neurons. Bladder (San Franc) 137 2287 PMID: 24934288

Abbas et al (2013) Directional summation in non-direction selective retinal ganglion cells. PLoS Comput Biol 9 e1002969 PMID: 23516351

Stark et al (2013) Inhibition-induced theta resonance in cortical circuits. Neuron 80 1263 PMID: 24314731

Zhang et al (2013) Molecular mechanisms that drive estradiol-dependent burst firing of Kiss1 neurons in the rostral periventricular preoptic area. Am J Physiol Endocrinol Metab 305 E1384 PMID: 24105416

Angelo and Margrie (2012) Population diversity and function of hyperpolarization-activated current in olfactory bulb mitral cells. Sci Rep 1 50 PMID: 22355569

Few et al (2012) Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release. Proc Natl Acad Sci U S A 109 E452 PMID: 22308469

Patel et al (2012) Frequency-selective exocytosis by ribbon synapses of hair cells in the bullfrog's amphibian papilla. Exp Physiol 32 13433 PMID: 23015434

Ma et al (2011) High purity human-induced pluripotent stem cell-derived cardiomyocytes: electrophysiological properties of action potentials and ionic currents. J Biomed Sci 301 H2006 PMID: 21890694

Goldberg et al (2011) Rapid developmental maturation of neocortical FS cell intrinsic excitability. J Neurosci 21 666 PMID: 20705896

Jung et al (2010) Downregulation of dendritic HCN channel gating in epilepsy is mediated by altered phosphorylation signaling. J Neurosci 30 6678 PMID: 20463230

Chen et al (2010) Homeostatic regulation of synaptic excitability: tonic GABA(A) receptor currents replace I(h) in cortical pyramidal neurons of HCN1 knock-out mice. J Neurosci 30 2611 PMID: 20164346

Ballo and Bucher (2009) Complex intrinsic membrane properties and dopamine shape spiking activity in a motor axon. J Neurosci 29 5062 PMID: 19386902

Bal and Baydas (2009) Electrophysiological properties of octopus neurons of the cat cochlear nucleus: an in vitro study. J Assoc Res Otolaryngol 10 281 PMID: 19277784

Zhang et al (2009) Developmental expression of a functional TASK-1 2P domain K+ channel in embryonic chick heart. J Neurosci 16 104 PMID: 19930646

Molineux et al (2008) Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons. Cereb Cortex 100 2684 PMID: 18768644

Lee and Ishida (2007) Ih without Kir in adult rat retinal ganglion cells. J Neurophysiol 97 3790 PMID: 17488978

Lee and Tepper (2007) A calcium-activated nonselective cation conductance underlies the plateau potential in rat substantia nigra GABAergic neurons. J Neurosci 27 6531 PMID: 17567814

Bender et al (2007) Localization of HCN1 channels to presynaptic compartments: novel plasticity that may contribute to hippocampal maturation. J Neurosci 27 4697 PMID: 17460082

Narushima et al (2007) Tonic enhancement of endocannabinoid-mediated retrograde suppression of inhibition by cholinergic interneuron activity in the striatum. PLoS One 27 496 PMID: 17234582

Angelo et al (2007) Local and global effects of I(h) distribution in dendrites of mammalian neurons. Am J Physiol Heart Circ Physiol 27 8643 PMID: 17687042

Hegg and Lucero (2004) Dopamine reduces odor- and elevated-K(+)-induced calcium responses in mouse olfactory receptor neurons in situ. J Neurophysiol 91 1492 PMID: 14657189

Doan et al (2004) Differential distribution and function of hyperpolarization-activated channels in sensory neurons and mechanosensitive fibers. Brain 24 3335 PMID: 15056713


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