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ZD 7288

Catalog #: 1000
55 Citations Datasheet / COA / SDS
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ZD 7288 | CAS No. 133059-99-1 | Ion Channel Modulators
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Description: Inhibits pacemaker (If) current
Alternative Names: ICI D7288

Chemical Name: 4-Ethylphenylamino-1,2-dimethyl-6-methylaminopyrimidinium chloride

Purity: ≥99%

Product Details
Citations (55)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

ZD 7288 is a sino-atrial node function modulator; blocks the hyperpolarization activated cation current If (HCN channel). Blocks Ih in central neurons. Increases NMDA-evoked noradrenaline release in rat brain in vitro.

Technical Data

M.Wt:
292.81
Formula:
C15H21ClN4
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
≥99%
Storage:
Desiccate at +4°C
CAS No:
133059-99-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. Hyperpolarization-activated cyclic nucleotide gated channels: a potential molecular link between epileptic seizures and Abeta generation in Alzheimer's disease.
    Saito Y, Inoue T, Zhu G, Kimura N, Okada M, Nishimura M, Kimura N, Murayama S, Kaneko S, Shigemoto R, Imoto K, Suzuki T
    Mol Neurodegener, 2012;7(0):50.
  3. Prolonging the postcomplex spike pause speeds eyeblink conditioning.
    Maiz, Jaione, Karakossian, Movses H, Pakaprot, Narawut, Robleto, Karla, Thompson, Richard, Otis, Thomas S
    Proc Natl Acad Sci U S A, 2012;109(41):16726-30.
  4. Dorsal BNST ?2A-adrenergic receptors produce HCN-dependent excitatory actions that initiate anxiogenic behaviors
    NA Harris, AT Isaac, A Günther, K Merkel, J Melchior, M Xu, E Eguakun, R Perez, BP Nabit, S Flavin, R Gilsbach, B Shonesy, L Hein, T Abel, A Baumann, R Matthews, SW Centanni, DG Winder
    J. Neurosci., 2018;0(0):.
  5. Pharmacological characterization of the inwardly rectifying current in the smooth muscle cells of the rat bladder.
    Green et al.
    Br.J.Pharmacol., 1996;119:1509
  6. Inhibitory actions of ZENECA ZD7288 on whole cell hyperpolarization activated inward current (If) in guinea-pig dissociated sinoatrial node cells.
    BoSmith et al.
    Br.J.Pharmacol., 1993;110:343
  7. Mechanism of block by ZD7288 of the hyperpolarization-activated inward rectifying current in guinea-pig substantia nigra neurons in vitro.
    Harris and Constanti
    J.Neurophysiol., 1995;74:2366
  8. Ih channels as modulators of presynaptic terminal function: ZD7288 increases NMDA-evoked [3H]-noradrenaline release in rat neocortex slices.
    Klar et al.
    Naunyn Schmiedebergs Arch.Pharmacol., 2003;367:422

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Citations for ZD 7288

The citations listed below are publications that use Tocris products. Selected citations for ZD 7288 include:

55 Citations: Showing 1 - 10

  1. Ketamine exerts its sustained antidepressant effects via cell-type-specific regulation of Kcnq2.
    Authors: Lopez Et al.
    Neuron  2022;110:2283
  2. Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation.
    Authors: Zhang Et al.
    Neuron  2018;98:918
  3. Reciprocal Circuits Linking the Prefrontal Cortex with Dorsal and Ventral Thalamic Nuclei.
    Authors: Collins Et al.
    Neuron  2018;98:366
  4. Soluble Aβ Oligomers Impair Dipolar Heterodendritic Plasticity by Activation of mGluR in the Hippocampal CA1 Region.
    Authors: Zhao Et al.
    iScience  2018;6:138
  5. Dorsal BNST α2A-Adrenergic Receptors Produce HCN-Dependent Excitatory Actions That Initiate Anxiogenic Behaviors.
    Authors: Harris Et al.
    J Neurosci  2018;38:8922
  6. Insights into the molecular mechanism for hyperpolarization-dependent activation of HCN channels.
    Authors: Flynn and Zagotta
    Proc Natl Acad Sci U S A  2018;115:E8086
  7. M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment.
    Authors: Lezmy
    Proc Natl Acad Sci U S A  2017;114(47):E10234
  8. Electrophysiological characterization of the M-current in rat hypoglossal motoneurons
    Authors: Ghezzi Et al.
    Neuroscience  2016;340:62
  9. Reduced Hyperpolarization-Activated Current Contributes to Enhanced Intrinsic Excitability in Cultured Hippocampal Neurons from PrP(-/-) Mice.
    Authors: Fan Et al.
    Front Cell Neurosci  2016;10:74
  10. Differential modulation of repetitive firing and synchronous network activity in neocortical interneurons by inhibition of A-type K(+) channels and Ih.
    Authors: Williams and Hablitz
    Front Cell Neurosci  2015;9:89
  11. Highly differentiated cellular and circuit properties of infralimbic pyramidal neurons projecting to the periaqueductal gray and amygdala.
    Authors: Ferreira Et al.
    PLoS One  2015;9:161
  12. A Cambrian origin for vertebrate rods.
    Authors: Asteriti Et al.
    Elife  2015;4
  13. Characterization of the role of HCN channels in β3-adrenoceptor mediated rat bladder relaxation.
    Authors: Kashyap Et al.
    Front Cell Neurosci  2015;2
  14. Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol.
    Authors: Merino Et al.
    J Neurophysiol  2015;10:e0132884
  15. Hcn1 is a tremorgenic genetic component in a rat model of essential tremor.
    Authors: Ohno Et al.
    J Neurosci  2015;10:e0123529
  16. Hyperpolarization-activated cyclic nucleotide-gated channels and cAMP-dependent modulation of exocytosis in cultured rat lactotrophs.
    Authors: Calejo Et al.
    J Neurosci  2014;34:15638
  17. DA modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels.
    Authors: Cilz Et al.
    Cereb Cortex  2014;24:3195
  18. Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra DA neurons.
    Authors: Dragicevic Et al.
    Bladder (San Franc)  2014;137:2287
  19. Directional summation in non-direction selective retinal ganglion cells.
    Authors: Abbas Et al.
    PLoS Comput Biol  2013;9:e1002969
  20. Contribution of d1/5 receptor modulation of post-spike/burst afterhyperpolarization to enhance neuronal excitability of layer v pyramidal neurons in prepubertal rat prefrontal cortex.
    Authors: Yi Et al.
    PLoS One  2013;8:e71880
  21. NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors.
    Authors: Zhang Et al.
    PLoS One  2013;8:e66122
  22. Inhibition-induced theta resonance in cortical circuits.
    Authors: Stark Et al.
    Neuron  2013;80:1263
  23. Molecular mechanisms that drive E2-dependent burst firing of Kiss1 neurons in the rostral periventricular preoptic area.
    Authors: Zhang Et al.
    Am J Physiol Endocrinol Metab  2013;305:E1384
  24. MPP(+) -dependent inhibition of Ih reduces spontaneous activity and enhances EPSP summation in nigral DA neurons.
    Authors: Masi Et al.
    Br J Pharmacol  2013;169:130
  25. Contribution of near-threshold currents to intrinsic oscillatory activity in rat medial entorhinal cortex layer II stellate cells.
    Authors: Boehlen Et al.
    J Neurophysiol  2013;109:445
  26. Frequency-selective exocytosis by ribbon synapses of hair cells in the bullfrog's amphibian papilla.
    Authors: Patel Et al.
    Exp Physiol  2012;32:13433
  27. Population diversity and function of hyperpolarization-activated current in olfactory bulb mitral cells.
    Authors: Angelo and Margrie
    Sci Rep  2012;1:50
  28. Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release.
    Authors: Few Et al.
    Proc Natl Acad Sci U S A  2012;109:E452
  29. High purity human-induced pluripotent stem cell-derived cardiomyocytes: electrophysiological properties of action potentials and ionic currents.
    Authors: Ma Et al.
    J Biomed Sci  2011;301:H2006
  30. Cyclic AMP signaling control of action potential firing rate and molecular circadian pacemaking in the suprachiasmatic nucleus.
    Authors: Atkinson Et al.
    J Biol Rhythms  2011;26:210
  31. Rapid developmental maturation of neocortical FS cell intrinsic excitability.
    Authors: Goldberg Et al.
    J Neurosci  2011;21:666
  32. Perineural dexmed. added to ropiva. for sciatic nerve block in rats prolongs the duration of analgesia by blocking the hyperpolarization-activated cation current.
    Authors: Brummett Et al.
    Anesthesiology  2011;115:836
  33. Electrophysiological effects of SKF83959 on hippocampal CA1 pyramidal neurons: potential mechanisms for the drug's neuroprotective effects.
    Authors: Chu Et al.
    PLoS One  2010;5
  34. Orchestration of "presto" and "largo" synchrony in up-down activity of cortical networks.
    Authors: Gullo Et al.
    Front Neural Circuits  2010;4:11
  35. Downregulation of dendritic HCN channel gating in epilepsy is mediated by altered phosphorylation signaling.
    Authors: Jung Et al.
    J Neurosci  2010;30:6678
  36. Homeostatic regulation of synaptic excitability: tonic GABA(A) receptor currents replace I(h) in cortical pyramidal neurons of HCN1 knock-out mice.
    Authors: Chen Et al.
    J Neurosci  2010;30:2611
  37. Complex intrinsic membrane properties and DA shape spiking activity in a motor axon.
    Authors: Ballo and Bucher
    J Neurosci  2009;29:5062
  38. Developmental expression of a functional TASK-1 2P domain K+ channel in embryonic chick heart.
    Authors: Zhang Et al.
    J Neurosci  2009;16:104
  39. Electrophysiological properties of octopus neurons of the cat cochlear nucleus: an in vitro study.
    Authors: Bal and Baydas
    J Assoc Res Otolaryngol  2009;10:281
  40. Low expression of Kv7/M channels facilitates intrinsic and network bursting in the developing rat hippocampus.
    Authors: Safiulina Et al.
    J Physiol  2008;586:5437
  41. Dynamic metabotropic control of intrinsic firing in cerebellar unipolar brush cells.
    Authors: Russo Et al.
    J Neurophysiol  2008;100:3351
  42. Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons.
    Authors: Molineux Et al.
    Cereb Cortex  2008;100:2684
  43. Ih without Kir in adult rat retinal ganglion cells.
    Authors: Lee and Ishida
    J Neurophysiol  2007;97:3790
  44. Local and global effects of I(h) distribution in dendrites of mammalian neurons.
    Authors: Angelo Et al.
    Am J Physiol Heart Circ Physiol  2007;27:8643
  45. A calcium-activated nonselective cation conductance underlies the plateau potential in rat substantia nigra GABAergic neurons.
    Authors: Lee and Tepper
    J Neurosci  2007;27:6531
  46. Tonic enhancement of endocannabinoid-mediated retrograde suppression of inhibition by cholinergic interneuron activity in the striatum.
    Authors: Narushima Et al.
    PLoS One  2007;27:496
  47. Localization of HCN1 channels to presynaptic compartments: novel plasticity that may contribute to hippocampal maturation.
    Authors: Bender Et al.
    J Neurosci  2007;27:4697
  48. Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons.
    Authors: Brager and Johnston
    J Neurosci  2007;27:13926
  49. Noradrenergic modulation of XII motoneuron inspiratory activity does not involve alpha2-receptor inhibition of the Ih current or presynaptic glutamate release.
    Authors: Adachi Et al.
    J Appl Physiol (1985)  2005;98:1297
  50. cAMP acts on exchange protein activated by cAMP/cAMP-regulated guanine nucleotide exchange protein to regulate transmitter release at the crayfish neuromuscular junction.
    Authors: Zhong and Zucker
    J Neurosci  2005;25:208
  51. DA reduces odor- and elevated-K(+)-induced calcium responses in mouse olfactory receptor neurons in situ.
    Authors: Hegg and Lucero
    J Neurophysiol  2004;91:1492
  52. HCN2 and HCN1 channels govern the regularity of autonomous pacemaking and synaptic resetting in globus pallidus neurons.
    Authors: Chan Et al.
    J Neurosci  2004;24:9921
  53. Differential distribution and function of hyperpolarization-activated channels in sensory neurons and mechanosensitive fibers.
    Authors: Doan Et al.
    Brain  2004;24:3335
  54. Frequency-dependent modulation of retinogeniculate transmission by serotonin.
    Authors: Seeburg Et al.
    J Neurosci  2004;24:10950
  55. Characterization of the human HCN1 channel and its inhibition by capsazepine.
    Authors: Gill Et al.
    Br J Pharmacol  2004;143:411

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